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Synthesis and topoisomerases inhibitory activity of heteroaromatic chalcones

Title
Synthesis and topoisomerases inhibitory activity of heteroaromatic chalcones
Authors
Jeon, Kyung-HwaYu, Han-BitKwak, Soo YeonKwon, YoungjooNa, Younghwa
Ewha Authors
권영주
SCOPUS Author ID
권영주scopus
Issue Date
2016
Journal Title
BIOORGANIC & MEDICINAL CHEMISTRY
ISSN
0968-0896JCR Link1464-3391JCR Link
Citation
vol. 24, no. 22, pp. 5921 - 5928
Keywords
Heteroaromatic chalconesTopoisomerases inhibitorsAnticancer activity
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
The critical role of nuclear topoisomerase enzymes during cell proliferation process guided topoisomerases to be one of the major targets for anticancer drug development. We have designed and synthesized 22 heteroaromatic ring incorporated chalcone derivatives substituted with epoxide or thioepoxide. Topoisomerase enzyme inhibitory activity and cytotoxic tests were also conducted to evaluate compounds' pharmacological efficacy. In the topoisomerase I inhibitory test, compound 1 was most active one, 24% of inhibition at 20 mu M, among all the compounds but it was lower than camptothecin. Compounds 9, 11, and 13 inhibited the function of topoisomerase II more strongly than etoposide with almost same magnitude (around 90% and 30% inhibition at 100 and 20 mu M, respectively) which were higher than those of etoposide (72% and 18% inhibition). In the cytotoxicity test, compound 9 inhibited T47D cancer cell growth with the IC50 value of 6.61 +/- 0.21. mu M. On the other hand, compound 13 (IC50: 4.32 +/- 0.18 mu M) effectively suppressed MDA-MB468 cancer cell growth. (C) 2016 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmc.2016.09.051
Appears in Collections:
약학대학 > 약학과 > Journal papers
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