Synthesis and SAR studies of 5-(pyridin-4-yl)-1, 3, 4-thiadiazol-2-amine derivatives as potent inhibitors of Bloom helicase

…, TS Dexheimer, O Gileadi, GH Nguyen, WK Chu…

Index: Rosenthal, Andrew S.; Dexheimer, Thomas S.; Gileadi, Opher; Nguyen, Giang H.; Chu, Wai Kit; Hickson, Ian D.; Jadhav, Ajit; Simeonov, Anton; Maloney, David J. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 20 p. 5660 - 5666

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Citation Number: 10

Abstract

Abstract Human cells utilize a variety of complex DNA repair mechanisms in order to combat constant mutagenic and cytotoxic threats from both exogenous and endogenous sources. The RecQ family of DNA helicases, which includes Bloom helicase (BLM), plays an important function in DNA repair by unwinding complementary strands of duplex DNA as well as atypical DNA structures such as Holliday junctions. Mutations of the BLM gene can ...