Synthesis and preliminary evaluation of curcumin analogues as cytotoxic agents

✍ Scribed by Qin Zhang; Ying Zhong; Lin-Na Yan; Xun Sun; Tao Gong; Zhi-Rong Zhang

• Publisher: Elsevier Science
• Year: 2011
• Tongue: English
• Weight: 488 KB
• Volume: 21
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/j.bmcl.2010.12.020

✦ Synopsis

A series of curcumin analogues with different substituents at the 4-position of the phenyl group were synthesized and screened for in vitro cytotoxicity against a panel of human cancer cell lines. Several novel curcumin analogues, especially 32 and 34, exhibited selective and potent cytotoxic activity against human epidermoid carcinoma cell line A-431 and human glioblastoma cell line U-251, implying their specific potential in the chemoprevention and chemotherapy of skin cancer and glioma. The preliminary SAR information extracted from the results suggested that introduction of appropriate substituents to the 4 0 -positions could be a promising approach for the development of new cytotoxic curcumin analogues with special selectivity for A-431 and U-251 cell lines.