Discovery of 1, 2, 4-thiadiazolidine-3, 5-dione analogs that exhibit unusual and selective rapid cell death kinetics against acute myelogenous leukemia cells in culture

S Nasim, ML Guzman, CT Jordan, PA Crooks

Index: Nasim, Shama; Guzman, Monica L.; Jordan, Craig T.; Crooks, Peter A. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 16 p. 4879 - 4883

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Citation Number: 4

Abstract

4-Benzyl-2-methyl-1, 2, 4-thiadiazolidine-3, 5-dione (TDZD-8) was previously identified as an antileukemic agent exhibiting no evident toxicity toward normal hematopoietic cells. An SAR study has been carried out to examine the effect of varying the C-2 and C-4- substituents on the thiadiazolidinone ring of TDZD-8 on antileukemic activity. These studies resulted in the identification of more druglike analogs that exhibited comparable potency ...