Novel fatty acid synthase (FAS) inhibitors: Design, synthesis, biological evaluation, and molecular docking studies

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• 作者：Xiaokui Wang ; Jian Lin ; Yao Chen ; Wu Zhong ; Guoming Zhao ; Hongying Liu ; Site Li ; Lili Wang ; Song Li
• 关键词：Fatty acid synthase inhibitors ; α ; -Methylene-β ; -carboxy-γ ; -thiobutyrolactones ; C75 analogs ; Synthesis
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2009
• 出版时间：1 March 2009
• 年：2009
• 卷：17
• 期：5
• 页码：1898-1904
• 全文大小：579 K

文摘

Several novel series of C75 derivatives were synthesized and evaluated for their FAS inhibitory activities. The results showed compound 4-methylene-2-octyl-5-oxo-tetrahydro-thiophene-3-carboxylic acid (1c) had more effective FAS inhibitory (IC₅₀ was 2.56 μM and T.I. was 9.26) and potent anti-tumor activities on HL60 and Hela cells in vitro (IC₅₀ were 5.38 μM and 46.10 μM, respectively).