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

Xiaokui Wang, Jian Lin, Yao Chen, Wu Zhong, Guoming Zhao, Hongying Liu, Site Li, Lili Wang, Song Li

Beijing Institute of Pharmacology and Toxicology, Beijing, PR China. wxkcaptain@yahoo.com.cn

Bioorganic & medicinal chemistry 2009 Mar 1

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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 (IC(50) was 2.56 microM and T.I. was 9.26) and potent anti-tumor activities on HL60 and Hela cells in vitro (IC(50) were 5.38 microM and 46.10 microM, respectively).

Citation

Xiaokui Wang, Jian Lin, Yao Chen, Wu Zhong, Guoming Zhao, Hongying Liu, Site Li, Lili Wang, Song Li. Novel fatty acid synthase (FAS) inhibitors: design, synthesis, biological evaluation, and molecular docking studies. Bioorganic & medicinal chemistry. 2009 Mar 1;17(5):1898-904