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Synthesis and in vitro anticancer activities of biotinylated derivatives of glaucocalyxin A and oridonin

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posted on 2020-05-22, 12:20 authored by Xiao-Lei Huang, Jing-Lei Chen, Xian-Lun Li, Lei Zhao, Ya-Dong Cui, Jiang-Yun Liu, Susan L. Morris-Natschke, Goto Masuo, Yung-Yi Cheng, Kuo-Hsiung Lee, Dao-Feng Chen, Jian Zhang

Fourteen glaucocalyxin A biotinylated derivatives, one glaucocalyxin C biotinylated derivative, and two oridonin biotinylated derivatives were designed and synthesized. Their structures were confirmed from 1H NMR, 13C NMR and HRMS data. The derivatives were evaluated for cytotoxic activities against lung (A549), cervical cancer cell line HeLa derivative (KB), multidrug-resistant KB subline (KB-VIN), triple-negative breast (MDA-MB-231), and estrogen receptor-positive breast (MCF-7) cancer cell lines.

Funding

This study was funded by the National Natural Science Foundation of China (grant number 81202882); the Social Development Project in Jiangsu Province of China (grant number BE2018322); the Priority Academic Program Development of the Jiangsu Higher Education Institutes, China (PAPD). Partial support was received from National Institutes of Health, NIH (grant number CA177584) awarded to Kuo-Hsiung Lee.

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