期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 7, 期 2, 页码 134-138出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.5b00272
关键词
SMYD3; oxindole; methyltransferase; KMT; oncology; tool compound
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.
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