Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.

doi:10.1016/j.bmcl.2011.04.060

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Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.

Bioorganic & medicinal chemistry letters - 15 Jun 2011

Thomas Mathew, Huang Wei-Sheng, Wen David, Zhu Xiaotian, Wang Yihan, Metcalf Chester A, Liu Shuangying, Chen Ingrid, Romero Jan, Zou Dong, Sundaramoorthi Raji, Li Feng, Qi Jiwei, Cai Lisi, Zhou Tianjun, Commodore Lois, Xu Qihong, Keats Jeff, Wang Frank, Wardwell Scott, Ning Yaoyu, Snodgrass Joseph T, Broudy Marc I, Russian Karin, Iuliucci John, Rivera Victor M, Sawyer Tomi K, Dalgarno David C, Clackson Tim, Shakespeare William C

Abstract excerpt

Ponatinib (AP24534) was previously identified as a pan-BCR-ABL inhibitor that potently inhibits the T315I gatekeeper mutant, and has advanced into clinical development for the treatment of refractory or resistant CML. In this study, we explored a novel series of five and six membered monocycles as alternate hinge-binding templates to replace the 6,5-fused imidazopyridazine core of ponatinib. Like ponatinib, these...

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PMID: 21561767
DOI: 10.1016/j.bmcl.2011.04.060

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