Norman Kong

TL;DR: In this article, the authors identify potent and selective small-molecule antagonists of MDM2 and confirm their mode of action through the crystal structures of complexes, leading to cell cycle arrest, apoptosis, and growth inhibition of human tumor xenografts.

TL;DR: In this paper, the authors provided a compound of formula I and the pharmaceutically acceptable salts and esters thereof, wherein X 1, X 2, R 1, R 2, R 3, R 4, R 5 and R 6 are described.

TL;DR: The recent understanding of the critical role of checkpoint kinase 1 (Chk1) in the G 2 checkpoint has generated great interest in the discovery of Chk1 inhibitors, which may represent a viable alternative target for cell cycle modulation.

TL;DR: RO4927350 is a potent and highly selective non-ATP-competitive MEK1/2 inhibitor with a novel chemical structure and unique mechanism of action that selectively blocks the MAPK pathway signaling both in vitro and in vivo, which results in significant antitumor efficacy in a broad spectrum of tumor models.

TL;DR: These efforts led to the discovery of benzoxazepinone 40, a potent BIR2-selective inhibitor with good in vivo pharmacokinetic properties which potentiates apoptotic signaling in a manner mechanistically distinct from that of known pan-IAP inhibitors.