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

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