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

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 mu M and T.I. was 9.26) and potent anti-tumor activities on HL60 and Hela cells in vitro (IC(50) were 5.38 mu M and 46.10 mu M, respectively). (C) 2009 Elsevier Ltd. All rights reserved.Biochemistry & Molecular BiologyChemistry, MedicinalChemistry, OrganicSCI(E)0ARTICLE51898-19041