Synthesis of curcumin derivatives targeting androgen receptor for castration‐resistant prostate cancer therapy

Author:

Liu Jiangfei1,Ni Yaohui1,Zhou Keyun1,Wu Guanzhao1,Hu Liangyong1,Zhu Tianyu1,Xu Defeng1ORCID,Hu Hang1ORCID

Affiliation:

1. School of Pharmacy Changzhou University Changzhou China

Abstract

AbstractIn this work, a series of curcumin derivatives (1a–1h, 2a–2g, and 3a–3c) were synthesized for the suppression of castration‐resistant prostate cancer cells. All synthesized compounds were characterized by 1H NMR, 13C NMR, HRMS, and melting point. The in vitro cytotoxicity study shows that compounds 1a, 1e, 1f, 1h, 2g, 3a, and 3c display similar or enhanced cytotoxicity against 22Rv1 and C4‐2 cells as compared to ASC‐J9, other synthesized compounds display reduced cytotoxicity against 22Rv1 and C4‐2 cells as compared to ASC‐J9. Molecular docking simulation was performed to study the binding affinity and probable binding modes of the synthesized compounds with androgen receptor. The results show that all synthesized compounds exhibit higher cdocker interaction energies as compared to ASC‐J9. Compounds 1h, 2g, and 3c not only show strong cytotoxicity against 22Rv1 and C4‐2 cells but also exhibit high binding affinity with androgen receptor. In androgen receptor suppression study, compounds 1f and 2g show similar androgen receptor suppression effect as compared to ASC‐J9 on C4‐2 cells, compound 3c displays significantly enhanced AR suppression effect as compared to ASC‐J9, 1f and 2g. Compounds 1a, 1e, 1f, 1h, 2g, 3a and 3c prepared in this work have significant potential for castration‐resistant prostate cancer therapy.

Publisher

Wiley

同舟云学术

1.学者识别学者识别

2.学术分析学术分析

3.人才评估人才评估

"同舟云学术"是以全球学者为主线,采集、加工和组织学术论文而形成的新型学术文献查询和分析系统,可以对全球学者进行文献检索和人才价值评估。用户可以通过关注某些学科领域的顶尖人物而持续追踪该领域的学科进展和研究前沿。经过近期的数据扩容,当前同舟云学术共收录了国内外主流学术期刊6万余种,收集的期刊论文及会议论文总量共计约1.5亿篇,并以每天添加12000余篇中外论文的速度递增。我们也可以为用户提供个性化、定制化的学者数据。欢迎来电咨询!咨询电话:010-8811{复制后删除}0370

www.globalauthorid.com

TOP

Copyright © 2019-2024 北京同舟云网络信息技术有限公司
京公网安备11010802033243号  京ICP备18003416号-3