Solution Phase Synthesis of a 3,5,7-Substituted Indolin-2-one Library as Potential CDK2 Inhibitor Isosteres

Author(s): Dmytro O. Tymoshenko, Brian T. Gregg, Matthew J. Hirsch, Jennifer L. Butcher

Journal Name: Letters in Drug Design & Discovery

Volume 5 , Issue 1 , 2008

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A set of 4-[N-(2-oxo-1,2-dihydro-indol-3-ylidene)-hydrazino]-benzamides focused on specific interactions at the ATP binding cleft of CDK2 was synthesized. The synthetic strategy towards potential inhibitors included the preparation of p-nitrophenyl activated esters and use of polymer scavengers to facilitate amide bond formation and purification. Using this methodology, a focused library of 244 compounds was prepared.

Keywords: ATP-competitive CDK inhibitor, Cyclin dependent kinases, hydrazones transformation, HPLC, hydrogen bond binding

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Article Details

Year: 2008
Page: [43 - 47]
Pages: 5
DOI: 10.2174/157018008783406633

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