Dataset Information

Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor.

ABSTRACT: SMYD3 has been implicated in a range of cancers; however, until now no potent selective small molecule inhibitors have been available for target validation studies. A novel oxindole series of SMYD3 inhibitors was identified through screening of the Epizyme proprietary histone methyltransferase-biased library. Potency optimization afforded two tool compounds, sulfonamide EPZ031686 and sulfamide EPZ030456, with cellular potency at a level sufficient to probe the in vitro biology of SMYD3 inhibition. EPZ031686 shows good bioavailability following oral dosing in mice making it a suitable tool for potential in vivo target validation studies.

SUBMITTER: Mitchell LH

PROVIDER: S-EPMC4753551 | biostudies-literature | 2016 Feb

REPOSITORIES: biostudies-literature

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Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor.

Mitchell Lorna H LH Boriack-Sjodin P Ann PA Smith Sherri S Thomenius Michael M Rioux Nathalie N Munchhof Michael M Mills James E JE Klaus Christine C Totman Jennifer J Riera Thomas V TV Raimondi Alejandra A Jacques Suzanne L SL West Kip K Foley Megan M Waters Nigel J NJ Kuntz Kevin W KW Wigle Tim J TJ Scott Margaret Porter MP Copeland Robert A RA Smith Jesse J JJ Chesworth Richard R

ACS medicinal chemistry letters 20150827 2

SMYD3 has been implicated in a range of cancers; however, until now no potent selective small molecule inhibitors have been available for target validation studies. A novel oxindole series of SMYD3 inhibitors was identified through screening of the Epizyme proprietary histone methyltransferase-biased library. Potency optimization afforded two tool compounds, sulfonamide EPZ031686 and sulfamide EPZ030456, with cellular potency at a level sufficient to probe the in vitro biology of SMYD3 inhibitio ...[more]

PMID: 26985287

Dataset Information

Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor.

Publications

Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor.

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