2. Academic Validation
  3. Discovery of novel N-hydroxy-2-arylisoindoline-4-carboxamides as potent and selective inhibitors of HDAC11

Discovery of novel N-hydroxy-2-arylisoindoline-4-carboxamides as potent and selective inhibitors of HDAC11

  • Bioorg Med Chem Lett. 2018 Jul 1;28(12):2143-2147. doi: 10.1016/j.bmcl.2018.05.021.
Matthew W Martin 1,  Jennifer Y Lee 2,  David R Lancia Jr 2,  Pui Yee Ng 2,  Bingsong Han 2,  Jennifer R Thomason 2,  Maureen S Lynes 2,  C Gary Marshall 2,  Chiara Conti 2,  Alan Collis 2,  Monica Alvarez Morales 2,  Kshama Doshi 2,  Aleksandra Rudnitskaya 2,  Lili Yao 3,  Xiaozhang Zheng 2
Affiliations

Affiliations

  • 1 FORMA Therapeutics, 500 Arsenal Street, Suite 100, Watertown, MA 02472, USA. Electronic address: mmartin@formatherapeutics.com.
  • 2 FORMA Therapeutics, 500 Arsenal Street, Suite 100, Watertown, MA 02472, USA.
  • 3 FORMA Therapeutics, 35 Northeast Industrial Road, Branford, CT 06405, USA.
PMID: 29776742 DOI: 10.1016/j.bmcl.2018.05.021
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; Hydroxamic acid; Inflammation; Isoindoline; Oncology.

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