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

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.