Design and synthesis of α-naphthoflavone chimera derivatives able to eliminate cytochrome P450 (CYP)1B1-mediated drug resistance via targeted CYP1B1 degradation

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成果类型：

期刊论文

作者：

Zhou, Li;Chen, Wenming;Cao, Chenyang;Shi, Yonghui;Ye, Wenchong;...

通讯作者：

Wang, LingLi;Zhou, W

作者机构：

[Zhou, Li] Hunan Agr Univ, Coll Sci, Furong Rd, Changsha 410128, Peoples R China.

[Chen, Wenming] Hunan Univ Chinese Med, Affiliated Hosp 1, Dept Pharmaceut, Prod Ctr, 95 Shaoshan Rd, Changsha 41007, Hunan, Peoples R China.

[Wang, LingLi; Zhou, Wen; Hu, Jiliang; Cao, Chenyang; Ye, Wenchong] Guangzhou Univ Chinese Med, Sch Pharmaceut Sci, E 232,Waihuan Rd, Guangzhou 510006, Peoples R China.

[Shi, Yonghui] Sun Yat Sen Univ, Sun Yat Sen Mem Hosp, Dept Pharm, Guangzhou 510120, Guangdong, Peoples R China.

通讯机构：

[Wang, LL; Zhou, W ] G

Guangzhou Univ Chinese Med, Sch Pharmaceut Sci, E 232,Waihuan Rd, Guangzhou 510006, Peoples R China.

语种：

英文

关键词：

CYP1B1;Click reaction;PROTACs;Reversal of drug resistance;alpha-Naphthoflavone-based conjugates

期刊：

European Journal of Medicinal Chemistry

ISSN：

0223-5234

年：

2020

卷：

189

页码：

112028

DOI：

10.1016/j.ejmech.2019.112028

基金类别：

The work is supported in part by financial support from National Natural Science Foundation of China (No. 21772028 ), Start-up Foundation of Guangzhou University of Chinese Medicine for Young scholar ( A1-AFD018171Z ), and General scientific research project of Guangzhou ( 201804010325 ). Appendix A

机构署名：

本校为第一机构

院系归属：

理学院

摘要：

Extrahepatic cytochrome P450 161 (CYP1B1), which is highly expressed in various tumors, is an attractive and potential target for cancer prevention, therapy, and reversal of drug resistance. CYP1B1 inhibition is the current predominant therapeutic paradigm to treating CYP1B1-mediated malignancy, but therapeutic effect has little success. Herein, we reported CYP1B1 degradation in place of CYP1BI inhibition for reversing drug resistance toward docetaxel in CYP1B1-overexpressing prostate cancer cell line DU145 using a PROTAC strategy. Replacing chlorine atom of a CYP1B1 selective inhibitor we fou...

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Design and synthesis of α-naphthoflavone chimera derivatives able to eliminate cytochrome P450 (CYP)1B1-mediated drug resistance via targeted CYP1B1 degradation

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