Le Wang

TL;DR: BCL-XL–selective inhibitors have the potential to enhance the efficacy of docetaxel in solid tumors and avoid the exacerbation of neutropenia observed with navitoclax, and demonstrate the translational utility of this toolkit of selective BCL-2 family inhibitors.

TL;DR: 4,5-Disubstituted imidazole was found to be the best for the replacement of the cis double bond in CA-4 and Medicinal chemistry efforts led to the discovery of compounds 24h and 25f that were finding to be 32 and 82% bioavailable, respectively, in rat.

TL;DR: A-1155463 caused a mechanism-based and reversible thrombocytopenia in mice and inhibited H146 small cell lung cancer xenograft tumor growth in vivo following multiple doses and represents an excellent tool molecule for studying BCL-XL biology as well as a productive lead structure for further optimization.

TL;DR: ABBV-744, a selective inhibitor of the BD2 domains of BET family proteins, is effective against prostate cancer in mouse xenograft models, with lower toxicities than the dual-bromodomain BET inhibitor ABBV -075 and underscores the potential value of selectively targeting theBD2 domain of BETfamily proteins for cancer therapy.

TL;DR: In this paper, compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-APOPotic BCL-2 protein.