Hudson, Liam published the artcileNovel Quinazolinone Inhibitors of ALK2 Flip between Alternate Binding Modes: Structure-Activity Relationship, Structural Characterization, Kinase Profiling, and Cellular Proof of Concept, Synthetic Route of 124341-06-6, the main research area is quinazolinone synthesis antitumor SAR ALK2 cancer.
Structure-activity relationship and crystallog. data revealed that quinazolinone-containing fragments flip between two distinct modes of binding to activin receptor-like kinase-2 (ALK2). We explored both binding modes to discover potent inhibitors and characterized the chem. modifications that triggered the flip in binding mode. We report kinase selectivity and demonstrate that compounds of this series modulate ALK2 in cancer cells. These inhibitors are attractive starting points for the discovery of more advanced ALK2 inhibitors.
Journal of Medicinal Chemistry published new progress about Homo sapiens. 124341-06-6 belongs to class bromides-buliding-blocks, name is 6-Amino-3-bromo-2-methylbenzoic acid, and the molecular formula is C8H8BrNO2, Synthetic Route of 124341-06-6.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary