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ID: ALA3091280

Journal: ACS Med Chem Lett

Title: Synthesis and Cytotoxicity of Semisynthetic Withalongolide A Analogues.

Authors: Motiwala HF, Bazzill J, Samadi A, Zhang H, Timmermann BN, Cohen MS, Aubé J.

Abstract: The natural product withaferin A exhibits potent antitumor activity and other diverse pharmacological activities. The recently discovered withalongolide A, a C-19 hydroxylated congener of withaferin A, was recently reported to possess cytotoxic activity against head and neck squamous cell carcinomas. Semisynthetic acetylated analogues of withalongolide A were shown to be considerably more cytotoxic than the parent compound. To further explore the structure-activity relationships, 20 new semisynthetic analogues of withalongolide A were synthesized and evaluated for cytotoxic activity against four different cancer cell lines. A number of derivatives were found to be more potent than the parent compound and withaferin A.

CiteXplore: 24273633

DOI: 10.1021/ml400267q