Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 2: Identification and optimisation of substituted 2,4-bis anilino pyrimidines

Bioorganic and Medicinal Chemistry Letters

Volumn 13, Issue 18, 2003, Pages 2961-2966

  Breault, Gloria A ^a   Ellston, Rebecca P A ^a   Green, Stephen ^a   James, S Russell ^a   Jewsbury, Philip J ^a   Midgley, Catherine J ^a   Pauptit, Richard A ^a   Minshull, Claire A ^a   Tucker, Julie A ^a   Pease, J Elizabeth ^a  

^a ASTRAZENECA   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

CYCLIN DEPENDENT KINASE 4; PROTEIN KINASE INHIBITOR; PYRIMIDINE DERIVATIVE;

ANTINEOPLASTIC ACTIVITY; ARTICLE; CANCER CHEMOTHERAPY; CHEMICAL MODIFICATION; DRUG IDENTIFICATION; DRUG POTENCY; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION; X RAY CRYSTALLOGRAPHY;

EID: 12444273643     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(03)00203-8     Document Type: Article

References (29)

1. Sherr C.J. Science. 274:1996;1672.
2. Barnes D.M., Gillet C.E. Breast Cancer Res. Treat. 52:1998;1.
3. Roussel M.F. Oncogene. 18:1999;5311.
4. Nevins J.R. Hum. Mol. Genet. 10:2001;699.
5. Tsao H., Benoit E., Sober A.J., Thiele C., Haluska F.G. Cancer Res. 58:1998;109.
6. Kimball S.D., Webster K.R. Annual Reports in Medicinal Chemistry. Doherty A.M. 2001;Academic, San Diego. Vol. 36 p 139, and references therein.
7. Ikuta M., Kamata K., Fukasawa K., Honma T., Machida T., Hirai H., Suzuki-Takahashi I., Hayama T., Nishimura S. J. Biol. Chem. 276:2001;27548.
8. Carini D.J., Kaltenbach R.F., Liu J., Benfield P.A., Boylan J., Boisclair M., Brizuela L., Burton C.R., Cox S., Grafstrom R., Harrison B.A., Harrison K., Akamike E., Markwalder J.A., Nakano Y., Seitz S.P., Sharp D.M., Trainor G.L., Sielecki T.M. Bioorg. Med. Chem. Lett. 11:2001;2209.
9. Honma T., Hayashi K., Aoyama T., Hashimoto N., Machida T., Fukasawa K., Iwama T., Ikeura C., Suzuki-Takahashi I. J. Med. Chem. 44:2001;4615.
10. Fry D.W., Bedford D.C., Harvey P.H., Fritsch A., Keller P.R., Wu Z., Dobrusin E., Leopold W.R., Fattaey A., Garrett M.D. J. Biol. Chem. 276:2001;16617.
11. Soni R., O'Reilly T., Furet P., Muller L., Stephan C., Zumstein-Mecker S., Fretz H., Fabbro D., Chaudhuri B. J. Natl. Cancer Inst. 93:2001;436.
12. Honma T., Yoshizumi T., Hashimoto N., Hayashi K., Kawanishi N., Fukasawa K., Takaki T., Ikeura C., Ikuta M., Suzuki-Takahashi I., Takashi H., Nishimura S., Morishima H. J. Med. Chem. 44:2001;4628.
13. Soni R., Muller L., Furet P., Schoepfer J., Stephan C., Zumstein-Mecker S., Fretz H., Chaudhuri B. Biochem. Biophys. Res. Commun. 275:2000;877.
14. Jeong H.-W., Kim M.-R., Son K.-H., Young Han M., Ha J.-H., Garnier M., Meijer L., Kwon B.-M. Bioorg. Med. Chem. Lett. 10:2000;1819.
15. Ryu C.-K., Kang H.-Y., Lee S.K., Nam K.A., Hong C.Y., Ko W.-G., Lee B.-H. Bioorg. Med. Chem. Lett. 10:2000;461.
16. Beattie, J. F.; Breault G. A.; Ellston, R. P. A.; Green S.; Jewsbury, P. J.; Midgely C. J.; Naven, R. T.; Pauptit, R.A.; Tucker, J. A.; Pease, J. E. Bioorg. Med. Chem. Lett. In press.
17. Breault, G. A.; Pease, J. E. PCT Int. Application WO 0012485 A1 20000309.
18. 25,26 have been deposited in the Protein Data Bank with deposition codes 1h01 and 1h08 together with structure factors and detailed experimental conditions.
19. Lawrie A.M., Noble M.E., Tunnah P., Brown N.R., Johnson L.N., Endicott J.A. Nat. Struct. Biol. 4:1997;796.
20. Legraverend M., Tunnah P., Noble M., Ducrot P., Ludwig O., Grierson D.S., Leost M., Meijer L., Endicott J. J. Med. Chem. 43:2000;1282.
21. Acta Crystallogr. D50:1994;760.
22. InsightII, Accelrys.
23. Quanta2000, Accelrys.
24. CNX version 2000.1, Accelrys.
25. 2.
26. 2.
27. Esnouf R. J. Mol. Graph. 15:1997;132.
28. Meritt E.A., Murphy M.E.P. Acta Crystallogr. D50:1994;869.
29. Bacon D., Anderson W.F. J. Mol. Graph. 6:1998;219.