Synthesis and bioevaluation of novel benzodipyranone derivatives as P-glycoprotein inhibitors for multidrug resistance reversal agents
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- 作者：Chien-Yu Chen ; Nai-Yu Liu ; Hui-Chang Lin ; Chih-Yu Lee ; Chin-Chuan Hung ; cc0206hung@gmail.com" class="auth_mail" title="E-mail the corresponding author ; Chih-Shiang Chang ; chihshiang@mail.cmu.edu.tw" class="auth_mail" title="E-mail the corresponding author
- 关键词：Multidrug resistance ; P-glycoprotein ; Benzodipyranone ; Reversal agent
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：8 August 2016
- 年：2016
- 卷：118
- 期：Complete
- 页码：219-229
- 全文大小：936 K
文摘
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The novel 52 benzodipyranone analogs were synthesized and evaluated for their P-gp inhibitory activity.
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Compound5a can enable the increase of the intracellular accumulation of P-gp substrate Calcein-AM.
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Compound5a exhibited more potency on promoted anticancer drugs cytotoxicity by reversing P-gp-mediated drug resistance.
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Compound5a can enhance the sensitization of resistant cell lines toward paclitaxel, vincristine, and doxorubicin.