Discovery of 4-(Benzylaminomethylene) isoquinoline-1, 3-(2 H, 4 H)-diones and 4-[(Pyridylmethyl) aminomethylene] isoquinoline-1, 3-(2 H, 4 H)-diones as Potent and …

…, J Kaplan, M Otteng, T Tran, K Kutterer…

Index: Tsou; Liu, Xiaoxiang; Birnberg, Gary; Kaplan, Joshua; Otteng, Mercy; Tran, Tritin; Kutterer, Kristina; Tang, Zhilian; Suayan, Ron; Zask, Arie; Ravi, Malini; Bretz, Angela; Grillo, Mary; Mcginnis, John P.; Rabindran, Sridhar K.; Ayral-Kaloustian, Semiramis; Mansour, Tarek S. Journal of Medicinal Chemistry, 2009 , vol. 52, # 8 p. 2289 - 2310

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Citation Number: 29

Abstract

The series of 4-(benzylaminomethylene) isoquinoline-1, 3-(2 H, 4 H)-dione and 4- [(pyridylmethyl) aminomethylene] isoquinoline-1, 3-(2 H, 4 H)-dione derivatives reported here represents a novel class of potential antitumor agents, which potently and selectively inhibit CDK4 over CDK2 and CDK1. In the benzylamino headpiece, a 3-OH substituent is required on the phenyl ring for CDK4 inhibitory activity, which is further enhanced when ...