1-Oxo-3-substitute-isothiochroman-4-carboxylic acid compounds: synthesis and biological activities of FAS inhibition.
A new series 1-oxo-3-substitute-isothiochroman-4-carboxylic acid compounds have been designed and synthesized. Screening of these molecules for FAS inhibition in vitro has indicated that compounds 2c and 2d showed more effective FAS inhibition activities and higher therapeutic index than C75.
Wang
Xiaokui
X
Beijing Institute of Pharmacology & Toxicology, Taiping Road 27, Beijing 100850, PR China.
Zhao
Guoming
G
Chen
Yao
Y
Xu
Xiaowei
X
Zhong
Wu
W
Wang
Lili
L
Li
Song
S
D019440:Anti-Obesity Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D002264:Carboxylic Acids / Q000737:chemistry*; D020134:Catalytic Domain; D002839:Chromans / Q000138:chemical synthesis* / Q000494:pharmacology; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000494:pharmacology; D064429:Fatty Acid Synthases / Q000037:antagonists & inhibitors*; D006801:Humans; D020128:Inhibitory Concentration 50; D007783:Lactones / Q000737:chemistry; D008956:Models, Chemical; D008958:Models, Molecular; D008968:Molecular Conformation; D017434:Protein Structure, Tertiary
D019440:Anti-Obesity Agents; D002264:Carboxylic Acids; D002839:Chromans; D004791:Enzyme Inhibitors; D007783:Lactones; D064429:Fatty Acid Synthases