2. Academic Validation
  3. Heterobiaryl purine derivatives as potent antiproliferative agents: inhibitors of cyclin dependent kinases. Part II

Heterobiaryl purine derivatives as potent antiproliferative agents: inhibitors of cyclin dependent kinases. Part II

  • Bioorg Med Chem Lett. 2009 Dec 1;19(23):6613-7. doi: 10.1016/j.bmcl.2009.10.011.
Michael P Trova 1,  Keith D Barnes,  Luis Alicea,  Travis Benanti,  Mark Bielaska,  Joseph Bilotta,  Brian Bliss,  Thuy Nguyen Duong,  Simon Haydar,  R Jason Herr,  Yu Hui,  Matthew Johnson,  John M Lehman,  Denise Peace,  Matthew Rainka,  Patricia Snider,  Susan Salamone,  Steven Tregay,  Xiaozhang Zheng,  Thomas D Friedrich
Affiliations

Affiliation

  • 1 AMRI, Medicinal Chemistry Department, 26 Corporate Circle, Albany, NY 12212-5098, USA.
PMID: 19854650 DOI: 10.1016/j.bmcl.2009.10.011
Abstract

C-6 Biarylmethylamino purine derivatives of roscovitine (1) inhibit cyclin dependent kinases and demonstrate potent antiproliferative activity. Replacement of the aryl rings of the C-6 biarylmethylamino group with heterobiaryl rings has provided compounds with significantly improved activity. In particular, derivatives 18 g and 9 c demonstrated 1000-fold and 1250-fold improvements, respectively, in the growth inhibition of HeLa cells compared to roscovitine (1).

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