European Journal of Medicinal Chemistry p. 445 - 469 (2019)
Update date:2022-08-15
Topics:
Ge, Weizhi
Hao, Xin
Han, Fangzhi
Liu, Zhongquan
Wang, Tianpeng
Wang, Mengmeng
Chen, Ning
Ding, Yahui
Chen, Yue
Zhang, Quan
Triple-negative breast cancer (TNBC) is the most aggressive cancers with a high recurrence rate and rapidly acquired drug resistance among various breast cancer subtypes. There is no specific drug for treatment of TNBC. Discovery of therapeutic agents with unique modes of actions is urgently needed. In this study, a series of seventy parthenolide derivatives was designed, synthesized, and evaluated for their anti-TNBC activities. Compound 7d exhibited the most potent activity against different breast cancer cells with IC50 values ranging from 0.20 μM to 0.27 μM, which demonstrated 11.6- to 18.6-fold improvement comparing to that of the parent compound parthenolide with IC50 values of 2.68–4.63 μM. It is worth to note that 7d was more active than the positive control drug ADR. Moreover, compound 7d could induce apoptosis of SUM-159 cells through mitochondria pathway and cause G1 phase arrest of SUM-159 cells. These findings indicate that compound 7d deserves further studies as a lead compound for ultimate discovery of effective anti-TNBC drug.
View MoreChangzhou Screw International Trading Co., Ltd.
Contact:13906149256,18001495888
Address:Jiangsu,Jintanqu
CGeneTech (Suzhou, China) Co., Ltd.
Contact:+86-512-62956962
Address:Room 101,Bld C11,218 Xinghu Rd.,Suzhou industrial Park
Chuzhou Baiao Biologhy S&T Co., Ltd.
Contact:+86-25-83212599;+86-25-83212699 13705185959
Address:Room 905, Tianzheng International Platza, No.399, Zhongyang Road ,Nanjing, Jiangsu Province, China
Wuhan Jadechem International Trade Co.,Ltd.
website:http://www.jadechem-intl.com
Contact:+86-27-83527060
Address:Room 502,Building C11,Software new city No.8,Huacheng Avenue,East Lake High-tech development zone,Wuhan,Hubei,China
Shanghai Yingrui Biopharma Co., Ltd
Contact:021-3358 8661*8003
Address:shanghai
Doi:10.1021/acs.joc.8b00983
(2018)Doi:10.1002/anie.202004652
(2020)Doi:10.1007/BF01158481
()Doi:10.1021/jo00946a025
(1973)Doi:10.1021/acs.orglett.5b02743
(2015)Doi:10.1039/P19720002067
(1972)