Article
Structure-based design of flavone-based inhibitors of wild-type and T315I mutant of ABL.
Bioorganic & medicinal chemistry letters - 1 Aug 2013
Choe Hyeonjeong, Kim Jieun, Hong Sungwoo
Abstract excerpt
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...
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