A to Z list - Northern Institute for Cancer Research

Professor Roger Griffin
Professor of Medicinal Chemistry

Email: roger.griffin@ncl.ac.uk
Telephone: +44 (0) 191 222 8591
Address: Northern Institute for Cancer Research
School of Natural Sciences-Chemistry
Bedson Building
University of Newcastle
Newcastle upon Tyne
NE1 7RU

Publications

Hardcastle IR, Liu J, Valeur E, Watson A, Ahmed SU, Blackburn TJ, Bennaceur K, Clegg W, Drummond C, Endicott JA, Golding BT, Griffin RJ, Gruber J, Haggerty K, Harrington RW, Hutton C, Kemp S, Lu X, McDonnell JM, Newell DR, Noble ME, Payne SL, Revill CH, Riedinger C, Xu Q, Lunec J. Isoindolinone Inhibitors of the Murine Double Minute 2 (MDM2)-p53 Protein-Protein Interaction: Structure-ActivityStudies Leading to Improved Potency. Journal of Medicinal Chemistry 2011, 54(5), 1233-1243.
Watson AF, Liu JF, Bennaceur K, Drummond CJ, Endicott JA, Golding BT, Griffin RJ, Haggerty K, Lu XH, McDonnell JM, Newell DR, Noble MEM, Revill CH, Riedinger C, Xu Q, Zhao Y, Lunec J, Hardcastle IR. MDM2-p53 protein-protein interaction inhibitors: A-ring substituted isoindolinones. Bioorganic & Medicinal Chemistry Letters 2011, 21(19), 5916-5919.
Saravanan K, Barlow HC, Barton M, Calvert AH, Golding BT, Newell DR, Northen JS, Curtin NJ, Thomas HD, Griffin RJ. Nucleoside Transport Inhibitors: Structure-Activity Relationships for Pyrimido[5,4-d]pyrimidine Derivatives That Potentiate Pemetrexed Cytotoxicity in the Presence of alpha(1)-Acid Glycoprotein. Journal of Medicinal Chemistry 2011, 54(6), 1847-1859.
Thomas HD, Wang LZ, Roche C, Bentley J, Cheng YZ, Hardcastle IR, Golding BT, Griffin RJ, Curtin NJ, Newell DR. Preclinical in vitro and in vivo evaluation of the potent and specific cyclin-dependent kinase 2 inhibitor NU6102 and a water soluble prodrug NU6301. European Journal of Cancer 2011, 47(13), 2052-2059.
Rodriguez SA, Clapham KM, Barrett L, Cano C, Desage ME, Griffin RJ, Hardcastle IR, Payne SL, Rennison T, Richardson C, Golding BT. Versatile Synthesis of Functionalised Dibenzothiophenes via Suzuki Coupling and Microwave-assisted Ring Closure. Organic & Biomolecular Chemistry 2011, 9(17), 6066-6074.
Rodriguez-Aristegui S, Clapham KM, Barrett L, Cano C, Desage-El Murr M, Griffin RJ, Hardcastle IR, Payne SL, Rennison T, Richardson C, Golding BT. Versatile synthesis of functionalised dibenzothiophenes via Suzuki coupling and microwave-assisted ring closure. Organic & Biomolecular Chemistry 2011, 9(17), 6066-6074.
Meschini E, Endicott JA, Golding BT, Hardcastle IR, Newell DR, Noble MEM, Wang LZ, Griffin RJ. Design and synthesis of dual CDK2 and CDK7 inhibitors. In: Abstracts of Papers of the American Chemical Society. 2010, American Chemical Society.
Clapham KM, Rennison T, Rodriguez-Aristegui S, Bardos J, Curtin NJ, Golding BT, Hardcastle IR, Newell DR, Cano C, Griffin RJ. Development of potent inhibitors of DNA-dependent protein kinase (DNA-PK). In: EJC Supplements: 22nd EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics. 2010, Berlin, Germany: Pergamon.
Carbain B, Roche C, Endicott JA, Golding BT, Hardcastle IR, Cano C, Zhen-Wang L, Newell DR, Noble MEM, Griffin RJ. Structure-based design of C8-substituted O6-alkylguanine CDK1 and 2 inhibitors. In: European Journal of Cancer Supplements: 22nd EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics. 2010, Berlin: Elsevier.
Thomas HD, Saravanan K, Wang LZ, Lin MJ, Northen JS, Barlow H, Barton M, Newell DR, Griffin RJ, Golding BT, Curtin NJ. Preclinical evaluation of a novel pyrimidopyrimidine for the prevention of nucleoside and nucleobase reversal of antifolate cytotoxicity. Molecular Cancer Therapeutics 2009, 8(7), 1828-1837.
Murr M, Cano C, Golding BT, Hardcastle IR, Hummersome M, Frigerio M, Curtin NJ, Menear K, Richardson C, Smith G, Griffin R. 8-Biarylchromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK). Bioorganic and Medicinal Chemistry Letters 2008, 18(17), 4885-4890.
Riedinger C, Endicott JA, Kemp SJ, Smyth LA, Watson A, Valeur E, Golding BT, Griffin RJ, Hardcastle IR, Noble ME, McDonnell JM. Analysis of Chemical Shift Changes Reveals the Binding Modes of Isoindolinone Inhibitors of the MDM2-p53 Interaction. Journal of the American Chemical Society 2008, 130(47), 16038-16044.
Willmore E, Elliott SL, Mainou-Fowler T, Summerfield GP, Jackson GH, O'Neill F, Lowe C, Carter A, Harris R, Pettitt AR, Cano-Soumillac C, Griffin RJ, Cowell IG, Austin CA, Durkacz BW. DNA-dependent protein kinase is a therapeutic target and an indicator of poor prognosis in B-cell chronic lymphocytic leukemia. Clinical Cancer Research 2008,14 12 3984-3992.
Lu X, Liu J, Watson A, Hardcastle IR, Griffin RJ, Golding BT, Newell DR, Lunec J. MDM2 and MDMX status as a determinant of in vitro cellular sensitivity to MDM2 antagonists in human tumour cell lines. EJC Supplements 2008, 6(12), 137.
Watson AF, Golding BT, Griffin RJ, Hutton C, Liu JF, Lug XH, Lunec J, Newell DR, Valeur E, Hardcastle IR. MEDI 147-Isoindolinone-based inhibitors of the MDM2-p53 protein-protein interaction. In: Abstracts of Papers of the American Chemical Society: 236th National Meeting of the American Chemical Society. 2008, Philadelphia, Pennsylvania, USA: American Chemical Society.
Seeberger S, Griffin RJ, Hardcastle IR, Golding BT. A new strategy for the synthesis of taurine derivatives using the 'safety-catch' principle for the protection of sulfonic acids. Organic & Biomolecular Chemistry 2007, 5(1), 132-138.
Hollick J, Rigoreau L, Cano-Soumillac C, Cockcroft X, Curtin NJ, Frigerio M, Golding BT, Guiard S, Hardcastle IR, Hickson I, Hummersone M, Menear K, Martin N, Matthews I, Newell DR, Ord R, Richardson C, Smith G, Griffin RJ. Pyranone, thiopyranone, and pyridone inhibitors of phosphatidylinositol 3-kinase related kinases. Structure-activity relationships for DNA-dependent protein kinase inhibition, and identification of the first potent and selective inhibitor of the ataxia telangiectasia mutated kinase. Journal of Medicinal Chemistry 2007,50 8 1958-1972.
Barbeau OR, Cano-Soumillac C, Griffin RJ, Hardcastle IR, Smith GCM, Richardson C, Clegg W, Harrington RW, Golding BT. Quinolinone and pyridopyrimidinone inhibitors of DNA-dependent protein kinase. Organic & Biomolecular Chemistry 2007, 5(16), 2670-2677.
Marchetti F, Sayle KL, Bentley J, Clegg W, Curtin NJ, Endicott JA, Golding BT, Griffin RJ, Haggerty K, Harrington RW, Mesguiche V, Newell DR, Noble MEM, Parsons RJ, Pratt DJ, Wang L, Hardcastle IR, Mesguiche V, Newell DR, Noble MEM, Parsons RJ, Pratt DJ, Wang L, Hardcastle IR. Structure-based design of 2-arylamino-4-cyclohexylmethoxy-5-nitroso-6- aminopyrimidine inhibitors of cyclin-dependent kinase 2. Organic and Biomolecular Chemistry 2007, 5(10), 1577-1585.
Aristegui SR, El-Murr MD, Golding BT, Griffin RJ, Hardcastle IR. Judicious application of allyl protecting groups for the synthesis of 2-morpholin-4-yl-4-oxo-4H-chromen-8-yl triflate, a key precursor of DNA-dependent protein kinase inhibitors. Organic Letters 2006, 8(26), 5927-5929.
Zhao Y, Thomas HD, Batey M, Cowell I, Richardson C, Griffin RJ, Calvert AH, Newell DR, Smith G, Curtin NJ. Preclinical evaluation of a potent novel DNA-dependent protein kinase inhibitor NU7441. Cancer Research 2006, 66(10), 5354-5362.
Griffin RJ, Henderson A, Curtin NJ, Echalier A, Endicott J, Hardcastle IR, Newell DR, Noble M, Wang L, Golding BT. Searching for cyclin-dependent kinase inhibitors using a new variant of the cope elimination. Journal of the American Chemical Society 2006, 128(18), 6012-6013.
Hardcastle, I.R., Ahmed, S., Atkins, H., Farnie, G., Golding, B.T., Griffin, R.J., Guyenne, S., Hutton,C., Källblad, P., Kemp, S., Kitching, M.S., Newell, D.R., Norbedo, S., Northen, J.S., Reid, R.J., Saravanan, K., Willems, H., Lunec, J. Small-molecule inhibitors of the MDM2-p53 protein-protein interaction based on an isoindolinone scaffold. Journal of Medicinal Chemistry 2006, 49(21), 6209-6221.
Barbeau OR, Golding BT, Griffin RJ, Hardcastle IR, Smith GCM, Richardson C. Design and synthesis of novel DNA-dependent protein kinase (DNA-PK) inhibitors. In: 230th National Meeting of the American Chemical Society. 2005, Washington, District of Columbia, USA: Abstracts of Papers of American Chemical Society: American Chemical Society.
Griffin RJ, Barbeau OR, Golding BT, Hardcastle IR, Smith GC, Richardson C. Design and synthesis of novel pyridopyrimidin-4-one and quinolin-4-one DNA-dependent protein kinase (DNA-PK) inhibitors. In: AACR/NCI/EORTC International Conference on Molecular Targets and Cancer Therapeutics. 2005, Philadelphia, Pennsylvania, USA: Clinical Cancer Research: American Association for Cancer Research.
Hardcastle I, Cockcroft X, Curtin NJ, El-Murr M, Leahy JJJ, Stockley M, Golding BT, Rigoreau L, Richardson C, Smith G, Griffin RJ. Discovery of potent chromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK) using a small-molecule library approach. Journal of Medicinal Chemistry 2005,48 24 7829-7846.
Fishel M, Newell D, Griffin R, Davison R, Wang L, Curtin NJ, Zuhowski E, Kasza K, Egorin M, Moschel R, Dolan M. Effect of cell cycle inhibition on cisplatin-induced cytotoxicity. Journal of Pharmacology and Experimental Therapeutics 2005,312 1 206-213.
Barbeau OR, Griffin RJ, Hardcastle IR, Golding BT. Efficient synthesis of 8-substituted 2-morpholine-4-yl-quinolin-4-ones: Potent inhibitors of DNA-dependent protein kinase. In: 230th National Meeting of the American Chemical Society. 2005, Washington, District of Columia, USA: Abstracts of The American Chemical Society: American Chemical Society.
Hardcastle, I.R., Ahmed, S.U., Barrett, P.A., Endicott, J.A., Golding, B.T., Griffin, R.J., Gruber, J., Hutton, C., Kemp, S.J., Lunec, J., Noble, M.E., Riedinger, C, Smyth, L.A. Inhibitors of the MDM2-p53 protein-protein interaction based on an isoindolinone scaffold. Clinical Cancer Research 2005, 11(24, Supplement 2), 9053.
Hardcastle I, Ahmed S, Atkins H, Calvert AH, Curtin NJ, Farnie G, Golding BT, Griffin R, Guyenne S, Hutton C, Källblad P, Kemp S, Kitching M, Newell D, Norbedo S, Northen J, Reid R, Saravanan K, Willems H, Lunec J. Isoindolinone-based inhibitors of the MDM2-p53 protein-protein interaction. Bioorganic and Medicinal Chemistry Letters 2005,15 5 1515-1520.
Griffin RJ, Henderson AJ, Cheng YZ, Curtin NJ, Endicott JA, Golding BT, Hardcastle IR, Newell DR, Noble ME, Wang LZ. Potent CDK2 inhibitors generated using a variant of the cope elimination. In: AACR/NCI/EORTC International Conference on Molecular Targets and Cancer Therapeutics. 2005, Philadelphia, Pennsylvania, USA: Clinical Cancer Research: American Association for Cancer Research.
Pennati M, Campbell AJ, Curto M, Binda M, Cheng Y, Wang L, Curtin NJ, Golding BT, Griffin RJ, Hardcastle IR, Henderson A, Zaffaroni N, Newell DR. Potentiation of paclitaxel-induced apoptosis by the novel cyclin-dependent kinase inhibitor NU6140: A possible role for survivin down-regulation. Molecular Cancer Therapeutics 2005,4 9 1328-1337.
Henderson A, Golding BT, Hardcastle IR, Griffin RJ. Searching for potent CDK inhibitors using a new variant of the Cope elimination. In: 230th National Meeting of the American Chemical Society. 2005, Washington, District of Columbia, USA: Abstracts of Papers of the American Chemical Society: American Chemical Society.
Henderson A, Cheng YZ, Curtin NJ, Endicott JA, Golding BT, Griffin RJ, Hardcastle IR, Newell DR, Noble MEM, Wang LZ. Searching for potent CDK2 inhibitors using a variant of the Cope elimination. In: 230th National Meeting of the American Chemical Society. 2005, Washington, District of Columbia, USA: Abstracts of Papers of The American Chemical Society: American Chemical Society.
Griffin RJ, Fontana G, Golding BT, Guiard SL, Hardcastle IR, Leahy JJJ, Martin N, Richardson C, Rigoreau LJM, Stockley ML, Smith GCM. Selective benzopyranone and pyrimido[2,1-alpha]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: Synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro. Journal of Medicinal Chemistry 2005, 48(2), 569-585.
Tikhe J, Webber S, Hostomsky Z, Maegley K, Ekkers A, Li J, Yu X, Almassy R, Kumpf R, Boritzki T, Zhang C, Calabrese C, Curtin NJ, Kyle S, Thomas HD, Wang L, Calvert AH, Golding B, Griffin RJ, Newell DR. Design, synthesis, and evaluation of 3,4-dihydro-2H-[1,4]diazepino[6,7,1- hi]indol-1-ones as inhibitors of poly(ADP-ribose) polymerase. Journal of Medicinal Chemistry 2004, 47(22), 5467-5481.
Leahy JJJ, Golding BT, Griffin RJ, Hardcastle IR, Richardson C, Rigoreau L, Smith GCM. Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries. Bioorganic & Medicinal Chemistry Letters 2004, 14(24), 6083-6087.
Hardcastle IR, Arris CE, Bentley J, Boyle FT, Chen Y, Curtin NJ, Endicott JA, Gibson AE, Golding BT, Griffin RJ, Jewsbury, P., Menyerol, J., Mesguiche, V., Newell, D.R., Noble, M., Pratt, D., Wang, L., Whitfield, H.J. N2-substituted O6-cyclohexylmethylguanine derivatives: Potent inhibitors of cyclin-dependent kinases 1 and 2. Journal of Medicinal Chemistry 2004, 47(15), 3710-3722.
White, A., Curtin, N.J., Eastman, B., Golding, B.T., Hostomsky, Z., Kyle,S., Li, J., Maegley, K., Skalitzky, D., Webber, S., Yu, X., Griffin, R.J. Potentiation of cytotoxic drug activity in human tumour cell lines, by amine-substituted 2-arylbenzimidazole-4-carboxamide PARP-1 inhibitors. Bioorganic and Medicinal Chemistry Letters 2004, 14(10), 2433-2437.
Curtin, N., Barlow, H., Bowman, K., Calvert, A. H., Davison, R., Golding, B., Huang, B., Loughlin, P., Newell, D., Smith, P., Griffin, R. Resistance-modifying agents. 11. Pyrimido[5,4-d]pyrimidine modulators of antitumor drug activity. Synthesis and structure-activity relationships for nucleoside transport inhibition and binding to α₁-acid glycoprotein. Journal of Medicinal Chemistry 2004, 47(20), 4905-4922.
Hollick JJ, Golding BT, Hardcastle IR, Martin N, Richardson C, Rigoreau LJM, Smith GCM, Griffin RJ. 2,6-disubstituted pyran-4-one and thiopyran-4-one inhibitors of DNA-dependent protein kinase (DNA-PK). Bioorganic & Medicinal Chemistry Letters 2003, 13(18), 3083-3086.
Mesguiche, V, Parsons, R.J., Arris, C.E., Bentley, J., Boyle, F., Curtin, N.J., Davies, T.G., Endicott, J., Gibson, A., Golding, B., Griffin, R.J., Jewsbury, P., Johnson, L.N., Newell, D.R., Noble, M.E.M., Wang, L., Hardcastle, I.R. 4-Alkoxy-2,6-diaminopyrimidine derivatives: Inhibitors of cyclin dependent kinases 1 and 2. Bioorganic and Medicinal Chemistry Letters 2003, 13(2), 217-222.
Whitfield HJ, Griffin RJ, Hardcastle IR, Henderson AP, Meneyrol J, Mesguiche V, Sayle KL, Golding BT. Facilitation of addition-elimination reactions in pyrimidines and purines using trifluoroacetic acid in trifluoroethanol. Chemical Communications 2003, (22), 2802-2803.
Sayle, K., Bentley, J., Boyle, F., Calvert, A. H., Cheng, Y., Curtin, N. J., Endicott, J., Golding, B., Hardcastle, I., Jewsbury, P., Mesguiche, V., Newell, D. R., Noble, M., Parsons, R., Pratt, D., Wang, L., Griffin, R. J. Structure-based design of 2-arylamino-4-cyclohexylmethyl-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinases 1 and 2. Bioorganic and Medicinal Chemistry Letters 2003, 13(18), 3079-3082.
Skalitzky, D., Marakovits, J., Maegley, K., Ekker, A., Yu, X., Hostomsky, Z., Webber, S., Eastman, B., Almassy, R., Li, J., Curtin, N. J., Newell, D. R., Calvert, A. H., Griffin, R. J., Golding, B. T. Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors. Journal of Medicinal Chemistry 2003, 46(2), 210-213.
Hollick JJ, Golding BT, Griffin RJ, Hardcastle IR, Leahy JJJ, Martin N, Rigoreau L, Smith GCM, Stockley ML. Application of combinatorial chemistry for the identification of pyran-4-one and thiopyran-4-one inhibitors of DNA-dependent protein kinase. In: 14th EORTC/NCI/AACR Symposium on Molecular Targets and Cancer Therapeutics. 2002, Frankfurt, Germany: European Journal of Cancer: Pergamon.
Raynaud FI, Smith NF, Griffin RJ, Hardcastle IR, Rigoreau LJM, Stockley ML, Leahy JJJ, Golding BT, Smith GC, Workman P. Cassette dosing iv and ip of novel DNA dependent protein kinase inhibitors. In: 14th EORTC/NCI/AACR Symposium on Molecular Targets and Cancer Therapeutics. 2002, Frankfurt, Germany: European Journal of Cancer: Pergamon.
Griffin RJ. Combinatorial methods for identifying antitumour kinase inhibitors. In: European Journal of Cancer: 14th EORTC/NCI/AACR Symposium on Molecular Targets and Cancer Therapeutics. 2002, Frankfurt, Germany: Pergamon.
Northen J, Boyle F, Clegg W, Curtin NJ, Edwards A, Griffin R, Golding B. Controlled stepwise conversion of 2,4,6,8-tetrachloropyrimido-[5,4-d ]pyrimidine into 2,4,6,8-tetrasubstituted pyrimido[5,4-d]pyrimidines. Journal of the Chemical Society. Perkin Transactions 1 2002,2 1 108-115.
Hardcastle IR, Golding BT, Griffin RJ. Designing inhibitors of cyclin-dependent kinases. Annual Review of Pharmacology and Toxicology 2002. , 42, 325-348.
Smith NF, Raynaud FI, Griffin RJ, Hardcastle IR, Rigoreau LJM, Stockley ML, Leahy JJJ, Golding BT, Martin N, Smith GCM, Workman P. High throughput pharmacokinetics of novel DNA-dependent protein kinase inhibitors. In: British Cancer Conference. 2002, Glasgow, UK: British Journal of Cancer: Nature Publishing Group.
Koch SSC, Thoresen LH, Tikhe JG, Maegley KA, Almassy RJ, Li JK, Yu XH, Zook SE, Kumpf RA, Zhang C, Boritzki TJ, Mansour RN, Zhang KE, Ekker A, Calabrese CR, Curtin NJ, Kyle S, Thomas HD, Wang LZ, Calvert AH, Golding BT, Griffin RJ, Newell DR, Webber SE, Hostomsky Z. Novel tricyclic poly(ADP-ribose) polymerase-1 inhibitors with potent anticancer chemopotentiating activity: Design, synthesis, and X-ray cocrystal structure. Journal of Medicinal Chemistry 2002, 45(23), 4961-4974.
Gibson A, Arris CE, Bentley J, Boyle F, Curtin NJ, Davies T, Endicott J, Golding BT, Grant S, Griffin R, Jewsbury, P., Johnson, L., Mesguiche, V., Newell, D.R., Noble, M., Tucker, J., Whitfield, H.J. Probing the ATP ribose-binding domain of cyclin-dependent kinases 1 and 2 with O6-substituted guanine derivatives. Journal of Medicinal Chemistry 2002, 45(16), 3381-3393.
Davies T, Bentley J, Arris CE, Boyle FT, Curtin NJ, Endicott J, Gibson A, Golding BT, Griffin RJ, Hardcastle IR, Jewsbury, P., Johnson, L., Mesguiche, V., Newell, D.R., Noble, M., Tucker, J.A., Wang, L., Whitfield, H.J. Structure-based design of a potent purine-based cyclin-dependent kinase inhibitor. Nature Structural Biology 2002, 9(10), 745-749.
Curtin NJ, Barton SB, Batey MA, Calabrese CR, Calvert AH, Durkacz BW, Griffin RJ, Golding BT, Kyle S, Newell DR, Thomas HD, Wang L, Almassy R, Boritzki T, Canan-Koch S, Hostomsky Z, Maegley K, Webber S. Anti-cancer chemosensitization in vitro and in vivo by a novel potent poly(ADP-ribose) polymerase (PARP1) inhibitor, TBI-361.. Clinical Cancer Research 2001, 7(11 Suppl.1), 88 S3740.
Smith PG, Thomas HD, Barlow HC, Griffin RJ, Golding BT, Calvert AH, Newell DR, Curtin NJ. In vitro and in vivo properties of novel nucleoside transport inhibitors with improved pharmacological properties that potentiate antifolate activity. Clinical Cancer Research 2001, 7(7), 2105-2113.
Farnie, G., Atkins, H., Calvert, A. H., Curtin, N. J., Golding, B. T., Griffin, R. J., Hardcastle, I. R., Kitching, M., Newell, D. R., Northen, J., Reid, R., Lunec, J. Inhibiting the MDM2-p53 interaction using low molecular weight compounds. British Journal of Cancer 2001, 85(Supplement 1), 81 no. 188.
Croughton KA, Matthews CS, Griffin RJ, Stevens MFG. Investigations on the biological properties of the lipophilic DHFR-inhibitory benzoprims reveal non-folate modes of action and opportunities for anti-cancer drug design. Anti-Cancer Drug Design 2001, 16(2), 119-128.
Veuger SJ, Durkacz BW, Golding BT, Griffin RJ, Martin N, Newell DR, Rigoreau LJM, Stockley ML, Webber SE, Hostomsky Z, Curtin NJ. Radiosensitization by novel inhibitors of PARP, PI, and DNA-PK, NU7026, in vitro. British Journal of Cancer 2001, 85(Supplement 1), 37.
Davies TG, Endicott JA, Noble ME, Johnson LN, Arris CE, Bentley J, Boyle FT, Calvert AH, Curtin NJ, Jewsberry PJ, Gibson AE, Golding BT, Griffin RJ, Hardcastle I, Mesguiche V, Parsons R, Whitfield H, Newell DR. Structural and thermodynamic validation of inactive cdk2 as a template for structure-based drug design. Cellular and Molecular Biology Letters 2001, 6(2B), 514-515.
Davies TG, Endicott JA, Johnson LN, Noble ME, Arris CE, Bentley J, Calvert AH, Curtin NJ, Golding BT, Griffin RJ, Hardcastle IH, Mesguiche V, Newell H, Parsons RJ, Whitfield HJ, Boyle T, Jewsbury P. Structure based design of a potent inhibitor of cdk2. Cellular and Molecular Biology Letters 2001, 6(2B), 470.
Stockley M, Clegg W, Fontana G, Golding BT, Martin N, Rigoreau LJM, Smith GCM, Griffin RJ. Synthesis, crystal structure determination, and biological properties of the DNA-dependent protein kinase (DNA-PK) inhibitor 3-cyano-6-hydrazonomethyl-5-(4-pyridyl)pyrid-[1H]-2-one (OK-1035). Bioorganic & Medicinal Chemistry Letters 2001, 11(21), 2837-2841.
Smith PG, Thomas HD, Barlow HC, Griffin RJ, Golding BT, Calvert AH, Newell DR, Curtin NJ. In vitro activity and in vivo pharmacology of two novel nucleoside transport inhibitors, NU3108 and NU3121. Clinical Cancer Research 2000, 6(Suppl. 1), 4555S-4555S.
Curtin, N. J., Calvert, A. H., Canan-Koch, S., Durkacz, B. W., Griffin, R. J., Golding, B. T., Hostomsky, Z., Kyle, S., Li, J., Maegley, K., Newell, D. R., Wang, L. Z., Webber, S. E., White, A., Yu, X. H. Chemopotentiation studies with two classes of potent (polyADP-ribose) polymerase (PARP) inhibitors in human lung and colon carcinoma cell lines.. Clinical Cancer Research 2000, 6(Supplement 1), 4507 no. 205.
Calabrese CR, Curtin NJ, Canan-Koch SS, Batey MA, Thomas HD, Kyle S, Wang LZ, Boritzki TJ, Webber SE, Griffin RJ, Golding BT, Hostomsky Z, Calvert AH, Newell DR. Design and evaluation of novel potent inhibitors of poly (ADP-ribose) polymerase. Clinical Cancer Research 2000, 6(Suppl. 1), 4496 No. 150.
Griffin RJ, Arris CE, Calvert AH, Curtin NJ, Jewsbury P, Endicott JA, Gibson AE, Boyle FT, Golding BT, Grant S, Johnson LN, Noble MEM, Newell DR, Lawrie A. Design, synthesis, and biological evaluation of O-6-alkylguanine and O-4-alkylpyrimidine cyclin-dependent kinase inhibitors. Abstracts of Papers of the American Chemical Society 2000, 219(2), U55 296-MEDI.
Arris CE, Boyle FT, Calvert AH, Curtin NJ, Endicott JA, Garman EF, Gibson AE, Golding BT, Grant S, Griffin RJ, Jewsbury P, Johnson LN, Lawrie AM, Newell DR, Noble MEM, Sausville EA, Schultz R, Yu W. Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles. Journal of Medicinal Chemistry 2000, 43(15), 2797-2804.
Arris, C. E., Boyle, F., Calvert, A. H., Curtin, N. J., Endicott, J. A., Garman, E. F., Gibson, A. E., Golding, B. T., Grant, S., Griffin, R. J., Jewsbury, P., Johnson, L., Lawrie, A., Newell, D. R., Noble, M., Sausville, E., Schultz, R., Yu, W. Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles. Journal of Medicinal Chemistry 2000, 43(15), 2797-2804.
Arris CE, Boyle FT, Calvert AH, Curtin NJ, Jewsbury P, Endicott JA, Gibson AE, Golding BT, Griffin RJ, Johnson LN, Laurie A, Yu W, Newell DR, Noble MEM, Sausville E, Schultz R, Garman EF, Grant S. O6-substituted guanines and 4-substituted pyrimidines: a novel class of antiproliferative cyclin dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles.. Journal of Medicinal Chemistry 2000, 43(15), 2797-2804.
Griffin, R. J., Arris, C. E., Bleasdale, C. , Boyle, F., Calvert, A. H., Curtin, N. J., Dalby, C., Kanugula, S., Lembicz, N., Newell, D. R., Pegg, A., Golding, B. T. Resistance-modifying agents. 8. Inhibition of O⁶-alkylguanine-DNA alkyltransferase by O⁶-alkenyl-, O⁶-cycloalkenyl-, and O⁶-(2-oxoalkyl)guanines and potentiation of temozolomide cytotoxicity in vitro by O⁶-(1-cyclopentenylmethyl) guanine. Journal of Medicinal Chemistry 2000, 43(22), 4071-4083.
White, A.W., Almassy, R., Calvert, A.H., Curtin, N.J., Griffin, R.J., Hostomsky, Z., Maegley, K., Newell, D.R., Srinivasan, S, Golding, B.T. Resistance-modifying agents. 9. Synthesis and biological properties of benzimidazole inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase. Journal of Medicinal Chemistry 2000, 43(22), 4084-4097.
Barlow, H. C., Bowman, K. J., Curtin, N. J., Calvert, A. H., Golding, B. T., Huang, B., Loughlin, P. J., Newell, D. R., Smith, P. G., Griffin, R. J. Resistance-modifying agents. Part 7: 2,6-Disubstituted-4,8-dibenzylaminopyrimido[5,4-d]pyrimidines that inhibit nucleoside transport in the presence of α1-acid glycoprotein (AGP). Bioorganic and Medicinal Chemistry Letters 2000, 10(6), 585-589.
Bentley J, Arris CE, Boyle FT, Calvert AH, Curtin NJ, Endicott JA, Gibson AE, Golding BT, Grant S, Griffin RJ, Jewsbury PJ, Johnson LN, Noble MEM, Newell DR. Structure-activity relationships and cellular effects of novel purine- and pyrimidine-based cyclin dependent kinase inhibitors. Clinical Cancer Research 2000, 6, 328.
Griffin, R. J., Barlow, H. C., Curtin, N. J., Calvert, A. H., Golding, B. T., Newell, D. R., Smith, P. G. 2,6-Disubstituted-4,8-dibenzylaminopyrimido[5,4-d]pyrimidines as nucleoside transport inhibitors: Structure-activity relationships for binding to alpha(1)-acid glycoprotein (AGP). Clinical Cancer Research 1999, 5(Supplement 1), 3843 no. 564.
Newell, D. R., Arris, C. E., Boyle, F. T., Calvert, A. H., Curtin, N. J., Dewsbury, P., Endicott, J. A., Garman, E. F., Gibson, A. E., Golding, B. T., Griffin, R. J., Johnson, L. N., Lawrie, A., Noble, M. E. M., Sausville, E. A., Schultz, R. Antiproliferative cyclin dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles. Clinical Cancer Research 1999, 5(Supplement 1), S3755 no. 124.
Arris CE, Boyle FT, Calvert AH, Curtin NJ, Dewsbury PJ, Endicott JA, Gibson AE, Golding BT, Grant S, Griffin RJ, Johnson, L. N., Noble, M. E. M., Newell, D. R., Sausville, E., Schultz, R. In vitro growth activity of novel purine- and pyrimidine-based CDK1 and CDK2 inhibitors. British Journal of Cancer 1999, 80(Supplement 2), 11 no. 110.
Smith, P. G., Barlow, H. C., Loughlin, P., Huang, B., Bowman, K. J., Calvert, A. H., Curtin, N. J., Golding, B. T., Griffin, R. J., Newell, D. R. Novel dipyridamole analogues potentiate the in vitro activity of MTA (LY231514) in the presence of alpha(1)-acid glycoprotein.. British Journal of Cancer 1999, 80(Supplement 2), 49 no. 82.
Curtin, N. J., Kyle, S., Wang, L. Z., Durkacz, B. W., White, A. J., Srinivasan, S., Griffin, R. J., Golding, B. T., Newell, D. R., Calvert, A. H., Maegley, K., Hostomsky, Z. Potentiation of temozolomide and topotecan growth inhibition by novel potent benzimidazole poly(ADP-ribose) polymerase (PARP) inhibitors. Clinical Cancer Research 1999, 5(Supplement 1), S3834 no. 520.
Curtin, N.J., Bowman, K., Turner, R., Huang, B., Loughlin, P., Calvert, A.H., Golding, B.T., Griffin, R.J., Newell, D.R. Potentiation of the cytotoxicity of thymidylate synthase (TS) inhibitors by dipyridamole analogues with reduced α1-acid glycoprotein binding. British Journal of Cancer 1999, 80(11), 1738-1746.
Calabrese CR, Thomas HD, Batey MA, Boritzki T, Zhang K, White AW, Curtin NJ, Griffin RJ, Golding BT, Hostomsky Z, Calvert AH, Newell DR. Preclinical pharmacology of novel substituted benzimidazoles - potent inhibitors of poly (ADP-ribose) polymerase. Clinical Cancer Research 1999, 5(Suppl. 1), S3839-S3839.
Almassy, R., Bowman, K., Calvert, A. H., Curtin, N. J., Golding, B. T., Hostomska, Z., Hostomsky, Z., Griffin, R. J., Maegley, K., Newell, D. R., Srinivasan, S., White, A. W., Webber, S. 2-phenylbenzimidazole-4-carboxamides are potent inhibitors of the DNA repair enzyme poly(ADP-ribose)-polymerase (PARP). In: 10th NCI-EORTC Symposium on New Drugs in Cancer Therapy. 1998, Amsterdam, The Netherlands: Annals of Oncology: Oxford University Press.
Robson C, Wright K, Twentyman P, Lambert P, Griffin R. Chemical synthesis and biological properties of novel fluorescent antifolates in Pgp- and MRP-overexpressing tumour cell lines. Biochemical Pharmacology 1998, 56(7), 807-816.
Endicott J, Noble M, Lawrie A, Tunnah P, Brown N, Johnson L, Calvert AH, Curtin NJ, Golding BT, Griffin RJ, Newell DR. Insights into CDK inhibitor design from X-ray crystallographic studies. In: 10th NCI-EORTC Symposium on New Drugs in Cancer Therapy. 1998, Amsterdam, The Netherlands: Annals of Oncology: Oxford University Press.
Grant S, Boyle F, Calvert AH, Curtin NJ, Endicott J, Golding BT, Griffin RJ, Johnson LN, Newell DR, Noble MEM, Robson CN. O-6-alkylguanines as selective inhibitors of cyclin dependent kinases. In: 10th NCI-EORTC Symposium on New Drugs in Cancer Therapy. 1998, Amsterdam, The Netherlands: Annals of Oncology: Oxford University Press.
Bowman, J., White, A.W., Golding, B.T., Griffin, R.J., Curtin, N.J. Potentiation of anti-cancer agent cytotoxicity by the potent poly(ADP-ribose) polymerase inhibitors NU1025 and NU1064. British Journal of Cancer 1998, 78(10), 1269-1277.
Griffin, R. J., Srinivasan, S., Bowman, K., Calvert, A. H., Curtin, N. J., Newell, D. R., Pemberton, L. C., Golding, B. T. Resistance-modifying agents. 5.1 Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP). Journal of Medicinal Chemistry 1998, 41(26), 5247-5256.
Robson C, Meek M, Grunwaldt J, Lambert P, Queener S, Schmidt D, Griffin R. Nonclassical 2,4-diamino-5-aryl-6-ethylpyrimidine antifolates: Activity as inhibitors of dihydrofolate reductase from Pneumocystis carinii and Toxoplasma gondii and as antitumor agents. Journal of Medicinal Chemistry 1997, 40(19), 3040-3048.
Griffin RJ, Gibson AE, Davison R, Irwin WJ. The 4-azidoberazyloxycarbonyl function; Application as a novel protecting group and potential prodrug modification for amines. Journal of the Chemical Society-Perkin Transactions 1, 11, 1205-1211 1996.
Arris, C. E., Bleasdale, C., Boyle, F. T., Calvert, A. H., Curtin, N. J., Dalby, C., Golding, B. T., Griffin, R. J., Lembicz, N., Lunn, J. M., Major, G. N., Newell, D. R. Mechanism-based inhibition of O-6-methylguanine-DNA methyltransferase.. Abstracts of Papers of the American Chemical Society 1996, 212(1), 99-TOXI.
Griffin, R.J., Srinivasan, S., White, A.W., Bowman, K., Calvert, A.H., Curtin, N.J., Newell, D.R., Golding, B.T. Novel benzimidazole and quinazolinone inhibitors of the DNA repair enzyme Poly(ADP-ribose)polymerase. Pharmaceutical Sciences 1996, 2(1), 43-47.
Griffin, R. J., Pemberton, L. C., Rhodes, D., Bleasdale, C., Bowman, K., Calvert, A. H., Curtin, N. J., Durkacz, B. W., Newell, D. R., Porteous, J. K., Golding, B. T. Novel potent inhibitors of the DNA-repair enzyme poly (ADP-ribose)polymerase (PARP). Anti-Cancer Drug Design 1995. , 10(6), 507-514.
Boulton, S., Pemberton, L. C., Porteous, J. K., Curtin, N. J., Griffin, R. J., Golding, B. T., Durkacz, B. W. Potentiation of temozolomide-induced cytotoxicity: a comparative study of the biological effects of poly(ADP-ribose) polymerase inhibitors.. British Journal of Cancer 1995, 72(4), 849-856.
Griffin RJ, Curtin NJ, Newell DR, Golding BT, Durkacz BW, Calvert AH. The Role of Inhibitors of Poly(Adp-Ribose) Polymerase as Resistance-Modifying Agents in Cancer-Therapy. Biochimie 1995, 77(6), 408-422.
Mitchinson A, Golding BT, Griffin RJ, O'Sullivan MC. Discrimination of spermidine amino functions by a new protecting group strategy; application to the synthesis of guanidinylated polyamines, including hirudonine. Journal of The Chemical Society. Chemical Communications 1994, (22), 2613-2614.
Arris, C. E., Bleasdale, C., Calvert, A. H., Curtin, N. J., Dalby, C., Golding, B. T., Griffin, R. J., Lunn, J. M., Major, G. N., Newell, D. R. Probing the active site and mechanism of action of O-6-methylguanine-DNA methyltransferase with substrate-analogs to (O-6-substituted guanines). Anti-Cancer Drug Design 1994, 9(5), 401-408.

Newcastle University

Northern Institute for Cancer Research

Professor Roger Griffin Professor of Medicinal Chemistry

Professor Roger Griffin
Professor of Medicinal Chemistry