University of California

University of Texas System

John B MacMillan

Charles G Caldwell

William H Fenical

Paul R Jensen

Doug E Frantz

Kevin H Gardner

James J LaClair

Richard Keith Bruick

Uttam K Tambar

Thomas H Scheuermann

Chambers C Hughes

Provided is a method of inhibiting heterodimerization of HIF-2&#x3b1; to HIF1&#x3b2; (ARNT) comprising binding certain small molecules to the HIF-2&#x3b1; PAS-B domain cavity but not to HIF1&#x3b1; and inhibiting HIF-2&#x3b1; heterodimerization to HIF1&#x3b2; (ARNT) but not inhibiting HIF1&#x3b1; heterodimerization to HIF1&#x3b2; (ARNT). Those certain small molecules are also referenced synonymously as HIF2-HDI and HIF2&#x3b1; heterodimerization inhibitors and also simply as certain small molecules.

Inhibition of HIF-2&#x3b1; heterodimerization with HIF1&#x3b2; (ARNT)

A compound having the general the general structure I is provided: (Formula I), wherein Z is a substituent selected from a group consisting of S and O; X is a substituent selected from a group consisting of Cl, Br, I, OH and NH2; each of Rand Ris a substituent independently selected from a group consisting of H, a linear, cyclic or branched, substituted or unsubstituted C-Calkyl, a substituted or unsubstituted aryl, and a substituted or unsubstituted heteroaryl; and each of Y and Yis a substituent independently selected from a group consisting of H and C(O)&#x2014;CH&#x2014;Br. 

Ammosamides as anticancer agents

Growing community of inventors

Dallas, TX, United States of America

John B MacMillan