期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 17, 期 5, 页码 1898-1904出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.01.050
关键词
Fatty acid synthase inhibitors; alpha-Methylene-beta-carboxy-gamma-thiobutyrolactones; C75 analogs; Synthesis
资金
- National Natural Science Foundation of China [30672534]
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 mu M and T.I. was 9.26) and potent anti-tumor activities on HL60 and Hela cells in vitro (IC50 were 5.38 mu M and 46.10 mu M, respectively). (C) 2009 Elsevier Ltd. All rights reserved.
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