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Molecules 2014, 19(11), 17256-17278;

Synthesis and Cytotoxic Evaluation of Alkoxylated Chalcones

Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
These authors contributed equally to this work.
Author to whom correspondence should be addressed.
Received: 25 July 2014 / Revised: 26 September 2014 / Accepted: 17 October 2014 / Published: 28 October 2014
(This article belongs to the Section Medicinal Chemistry)
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A series of chalcones a120 bearing a 4-OMe groups on the A-ring were initially synthesized and their anticancer activities towards HepG2 cells evaluated. Subsequently, a series of chalcones b142 bearing methoxy groups at the 2' and 6'-positions of the B-ring were synthesized and their anticancer activities towards five human cancer cell lines (HepG2, HeLa, MCF-7, A549 and SW1990) and two non-tumoral human cell lines evaluated. The results showed that six compounds (b6, b8, b11, b16, b18, b22, b23 and b29) displayed promising activities, with compounds b22 and b29 in particular showing higher levels of activity than etoposide against all five cancer cell lines. Compound b29 showed a promising SI value compared with both HMLE and L02 (2.1–6.5 fold in HMLE and > 33 > 103.1 fold in L02, respectively). View Full-Text
Keywords: alkoxylated chalcones; synthesis; cytotoxicity alkoxylated chalcones; synthesis; cytotoxicity

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Bai, X.-G.; Xu, C.-L.; Zhao, S.-S.; He, H.-W.; Wang, Y.-C.; Wang, J.-X. Synthesis and Cytotoxic Evaluation of Alkoxylated Chalcones. Molecules 2014, 19, 17256-17278.

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