Bioorganic & medicinal chemistry letters

Structure-based design of flavone-based inhibitors of wild-type and T315I mutant of ABL

H Choe, J Kim, S Hong

Index: Choe, Hyeonjeong; Kim, Jieun; Hong, Sungwoo Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 15 p. 4324 - 4327

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Citation Number: 2

Abstract

The existence of drug resistance caused by mutations in the break-point cluster region- Abelson (BCR-ABL) tyrosine kinase domain remains a clinical challenge due to limited treatment options for effective CML therapies. Here, we report a series of flavone-based common inhibitors equipotent for the wild type and the most drug-resistant T315I mutant of BCR-ABL. The original hit 1 was extensively modified through a structure-based drug ...