Solution Phase Synthesis of a 3,5,7-Substituted Indolin-2-one Library as Potential CDK2 Inhibitor Isosteres
Dmytro O. Tymoshenko,
Brian T. Gregg,
Matthew J. Hirsch,
Jennifer L. Butcher.
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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