Abstract
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
Letters in Drug Design & Discovery
Title: Solution Phase Synthesis of a 3,5,7-Substituted Indolin-2-one Library as Potential CDK2 Inhibitor Isosteres
Volume: 5 Issue: 1
Author(s): Dmytro O. Tymoshenko, Brian T. Gregg, Matthew J. Hirsch and Jennifer L. Butcher
Affiliation:
Keywords: ATP-competitive CDK inhibitor, Cyclin dependent kinases, hydrazones transformation, HPLC, hydrogen bond binding
Abstract: 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.
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Cite this article as:
Tymoshenko O. Dmytro, Gregg T. Brian, Hirsch J. Matthew and Butcher L. Jennifer, Solution Phase Synthesis of a 3,5,7-Substituted Indolin-2-one Library as Potential CDK2 Inhibitor Isosteres, Letters in Drug Design & Discovery 2008; 5 (1) . https://dx.doi.org/10.2174/157018008783406633
DOI https://dx.doi.org/10.2174/157018008783406633 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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