期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 12, 页码 3912-3915出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.04.108
关键词
Adipocyte; Aldol condensation; Chalcone; Diabetes; Structure-activity relationship
资金
- National Science Council, Taiwan [NSC 98-2323-B-037-004-, 99-2323-B-037-002-]
Chalcones bearing electron donating or electron withdrawing substitutions were prepared and their glucose uptake activity was evaluated. Chalcone derivatives were synthesized in one step protocol with high purity and yield. Chalcones with chloro, bromo, iodo and hydroxy substitutions at position 2 on A-ring exhibited the highest activity with glucose medium concentration (210 to 236 mg/dl) compared to pioglitazone and rosiglitazone (230 and 263 mg/dl, respectively). Also chalcones with iodo substitution at position 3 on A-ring were comparably active (<= 238 mg/dl). The structure-activity relationship of the tested chalcones was studied and the findings were supported statistically (C) 2012 Elsevier Ltd. All rights reserved.
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