Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles.

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, ME; Sausville, EA; Schultz, R; Yu, W

Abstract:

Substituted guanines and pyrimidines were tested as inhibitors of cyclin B1/CDK1 and cyclin A3/CDK2 and soaked into crystals of monomeric CDK2. O6-Cyclohexylmethylguanine (NU2058) was a competitive inhibitor of CDK1 and CDK2 with respect to ATP (Ki values: CDK1, 5 +/- 1 microM; CDK2, 12 +/- 3 microM) and formed a triplet of hydrogen bonds (i.e., NH-9 to Glu 81, N-3 to Leu 83, and 2-NH2 to Leu 83). The triplet of hydrogen bonding and CDK inhibition was reproduced by 2,6-diamino-4-cyclohexylmet...

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APA Style

Arris, C. E., Boyle, F. T., 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. N., Lawrie, A. M., Newell, D. R., Noble, M. E., Sausville, E. A., Schultz, R., & Yu, W. (2000). Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles. Journal of Medicinal Chemistry, 43(15), 2797–2804.

MLA Style

Arris, C. E., et al. “Identification of Novel Purine and Pyrimidine Cyclin-Dependent Kinase Inhibitors with Distinct Molecular Interactions and Tumor Cell Growth Inhibition Profiles.” Journal of Medicinal Chemistry, vol. 43, no. 15, Journal of medicinal chemistry, 2000, pp. 2797–804.

Chicago Style

Arris, CE, FT Boyle, AH Calvert, NJ Curtin, JA Endicott, EF Garman, AE Gibson, et al. 2000. “Identification of Novel Purine and Pyrimidine Cyclin-Dependent Kinase Inhibitors with Distinct Molecular Interactions and Tumor Cell Growth Inhibition Profiles.” Journal of Medicinal Chemistry 43 (15): 2797–2804.
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