國家衛生研究院 NHRI:Item 3990099045/12367

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Title:	Design, synthesis and anticancer evaluation of beta-carboline-1-one hydantoins
Other Titles:	Design, synthesis and anticancer evaluation of β-carboline-1-one hydantoins
Authors:	Yao, CH;Hsieh, TC;Song, JS;Lee, JC
Contributors:	Institute of Biotechnology and Pharmaceutical Research
Abstract:	Aim: Cancer is a major health burden and a leading cause of death worldwide. We sought to discover potential anticancer molecules with novel scaffold for further development of more active agents to address the issue. Methodology: A series of beta-carboline-1-one hydantoins were designed according to a conformational restriction strategy, synthesized via a one-pot Knoevenagel condensation-intramolecular cyclization, and tested in cytotoxicity assays. Results: The study culminated in the identification of 6b and 6c, both of which were found to potently inhibit breast and lung cancer cell lines. Of particular interest was 6c, which was 83 times more potent an inhibitor than 5-fluorouracil in inhibiting MCF-7. Conclusion: This work establishes beta-carboline-1-one hydantoin as a promising scaffold in the investigation of anticancer agents.
Date:	2020-02
Relation:	Future Medicinal Chemistry. 2020 Feb;12(3):183-192.
Link to:	http://dx.doi.org/10.4155/fmc-2019-0276
JIF/Ranking 2023:	http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=1756-8919&DestApp=IC2JCR
Cited Times(WOS):	https://www.webofscience.com/wos/woscc/full-record/WOS:000525278100003
Cited Times(Scopus):	https://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85079249667
Appears in Collections:	[Jinq-Chyi Lee] Periodical Articles

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