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Mar. Drugs 2018, 16(4), 133;

Recent Synthesis and Discovery of Brefeldin A Analogs

College of Pharmacy and Research Institute of Pharmaceutical Sciences, Gyeongsang National University, Jinju daero 501, Jinju, Gyeongnam 52828, Korea
Received: 13 March 2018 / Revised: 6 April 2018 / Accepted: 11 April 2018 / Published: 18 April 2018
(This article belongs to the Special Issue Connection of Marine Natural Products and Cell Apoptosis)
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The recent development of analogs of brefeldin A (BFA), a fungal metabolite, for the improvement of BFA apoptosis-inducing activity is described. BFA has been isolated from various soil or, more recently, marine fungi and has shown versatile beneficial activities. More importantly, the apoptosis-inducing activity of BFA in cancer cells highlights the possibility of further developing this natural product as an anticancer agent. Besides its biological importance, its structural features have also gathered tremendous interest from both medicinal and synthetic chemists. By a medicinal chemistry and total synthesis approach, numerous analogs from BFA have been developed to improve its inferior bioavailability and its antiproliferative ability. In this review, the recent medicinal chemistry efforts in relation to the production of BFA analogs are extensively presented. View Full-Text
Keywords: brefeldin A; medicinal chemistry; apoptosis; anticancer agent brefeldin A; medicinal chemistry; apoptosis; anticancer agent

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Paek, S.-M. Recent Synthesis and Discovery of Brefeldin A Analogs. Mar. Drugs 2018, 16, 133.

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