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Discovery of novel N-hydroxy-2-arylisoindoline-4-carboxamides as potent and selective inhibitors of HDAC11 |
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| Authors: | Matthew W. Martin Jennifer Y. Lee David R. Lancia Pui Yee Ng Bingsong Han Jennifer R. Thomason Maureen S. Lynes C. Gary Marshall Chiara Conti Alan Collis Monica Alvarez Morales Kshama Doshi Aleksandra Rudnitskaya Lili Yao Xiaozhang Zheng |
| Affiliation: | 1. FORMA Therapeutics, 500 Arsenal Street, Suite 100, Watertown, MA 02472, USA;2. FORMA Therapeutics, 35 Northeast Industrial Road, Branford, CT 06405, USA |
| Abstract: | N-Hydroxy-2-arylisoindoline-4-carboxamides are potent and selective inhibitors of HDAC11. The discovery, synthesis, and structure activity relationships of this novel series of inhibitors are reported. An advanced analog (FT895) displays promising cellular activity and pharmacokinetic properties that make it a useful tool to study the biology of HDAC11 and its potential use as a therapeutic target for oncology and inflammation indications. |
| Keywords: | HDAC11 HDACs Oncology Inflammation Isoindoline Hydroxamic acid |
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