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Synthesis of 2-methoxybenzamide derivatives and evaluation of their hedgehog signaling pathway inhibition. 2021

Chiyu Sun, and Dajun Zhang, and Tian Luan, and Youbing Wang, and Wenhu Zhang, and Lin Lin, and Meihua Jiang, and Ziqian Hao, and Ying Wang
School of Pharmacy, Shenyang Medical College Shenyang 110034 China scy_dream@126.com.

Aberrant hedgehog (Hh) signaling is implicated in the development of a variety of cancers. Smoothened (Smo) protein is a bottleneck in the Hh signal transduction. The regulation of the Hh signaling pathway to target the Smo receptor is a practical approach for development of anticancer agents. We report herein the design and synthesis of a series of 2-methoxybenzamide derivatives as Hh signaling pathway inhibitors. The pharmacological data demonstrated that compound 21 possessed potent Hh pathway inhibition with a nanomolar IC50 value, and it prevented Shh-induced Smo from entering the primary cilium. Furthermore, mutant Smo was effectively suppressed via compound 21. The in vitro antiproliferative activity of compound 21 against a drug-resistant cell line gave encouraging results.

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