Article
First SAR Study for Overriding NRAS Mutant Driven Acute Myeloid Leukemia.
Journal of medicinal chemistry - 27 Sept 2018
Cho Hanna, Shin Injae, Ju Eunhye, Choi Seunghye, Hur Wooyoung, Kim Haelee, Hong Eunmi, Kim Nam Doo, Choi Hwan Geun, Gray Nathanael S, Sim Taebo
Abstract excerpt
GNF-7, a multitargeted kinase inhibitor, served as a dual kinase inhibitor of ACK1 and GCK, which provided a novel therapeutic strategy for overriding AML expressing NRAS mutation. This SAR study with GNF-7 derivatives, designed to target NRAS mutant-driven AML, led to identification of the extremely potent inhibitors, 10d, 10g, and 11i, which possess single-digit nanomolar inhibitory activity against both ACK1...
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