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

X Wang, J Lin, Y Chen, W Zhong, G Zhao, H Liu…

Index: Wang, Xiaokui; Lin, Jian; Chen, Yao; Zhong, Wu; Zhao, Guoming; Liu, Hongying; Li, Site; Wang, Lili; Li, Song Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 5 p. 1898 - 1904

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Citation Number: 19

Abstract

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 TI 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).