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Toogood, P.L. et al.

Toogood, Harvey, Repine, Sheehan, VanderWel, Zhou, Keller, McNamara, Sherry, Zhu, Brodfuehrer, Choi, Barvian, Fry,

Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6.

A pharmacological approach to inhibition of cyclin-dependent kinases 4 and 6 (Cdk4/6) using highly selective small molecule inhibitors has the potential to provide novel cancer therapies for clinical use. Achieving high levels of selectivity for Cdk4/6, versus other ATP-dependent kinases, presents a significant challenge. The pyrido[2,3-d]pyrimidin-7-one template provides an effective platform for the inhibition of a broad cross-section of kinases, including Cdks. It is now demonstrated that the modification of pyrido[2,3-d]pyrimidin-7-ones to include a 2-aminopyridine side chain at the C2-position provides inhibitors with exquisite selectivity for Cdk4/6 in vitro. This selectivity profile is recapitulated in cells where the most selective inhibitors create a G(1) block at concentrations up to 100-fold the IC(50) for cell proliferation. On the basis of its selectivity profile and pharmacokinetic profile, compound 43 (PD 0332991) was identified as a drug candidate for the treatment of cancer.[1]

References

Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6. Toogood, P.L., Harvey, P.J., Repine, J.T., Sheehan, D.J., VanderWel, S.N., Zhou, H., Keller, P.R., McNamara, D.J., Sherry, D., Zhu, T., Brodfuehrer, J., Choi, C., Barvian, M.R., Fry, D.W. J. Med. Chem. (2005) [Pubmed]

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