MedChemComm p. 1036 - 1042 (2015)
Update date:2022-08-04
Topics:
Luo, Yong
Zhu, Yongxia
Ran, Kai
Liu, Zhihao
Wang, Ningyu
Feng, Qiang
Zeng, Jun
Zhang, Lidan
He, Bing
Ye, Tinghong
Zhu, Shirui
Qiu, Xiaolong
Yu, Luoting
In this study, a series of novel N-(4-phenylthiazol-2-yl)cinnamamide derivatives (7a-8n) were synthesized and evaluated for their anti-proliferative activities in vitro by MTT assay and a possible antitumor mechanism was also explored. SAR analysis showed that steric effects played an important role on the anti-tumor activity. The most potent analogue 8f showed excellent inhibitions on the K562, Bel7402, A549 and Jurkat cells ranging from sub-micromolar to nanomolar concentration. Compound 8f inhibited Jurkat cells with an IC50 value of 0.035 μM with no apparent toxicity in different non-cancerous cells. Furthermore, it was suggested that the possible mechanism of 8f might be associated with inducing cancer cell apoptosis following flow cytometer analysis and Hoechst 33358 staining assays.
View MoreShanghai Standard Biotech Co., Ltd.
Contact:+86-18502101150
Address:Room 103, Building 2nd, NO.720, Cailun Road , Pudong District, Shanghai, China
Hunan Shineway Enterprise Co., Ltd.
Contact:+86-731-86303875
Address:118, Huanghua International Airport Road, Huanghua Town, Changsha, Hunan 410137, China
Changsha Yonta Industry Co., Ltd.
Contact:+ 86-731-8535 2228
Address:Rm.1717, North Bldg., No.368, East 2nd Ring Road(2nd Section)
Contact:+86-519-86623222
Address:29F/D, 99 Yanling West Road, Changzhou, Jiangsu, China
website:http://www.sigmaaldrich.com
Contact:800 558-9160
Address:Industriestrasse 25CH-9471 Buchs SGSwitzerland
Doi:10.1246/bcsj.47.3102
(1974)Doi:10.1039/c9cc07184a
(2019)Doi:10.1016/j.tet.2006.12.059
(2007)Doi:10.1016/j.tet.2020.131313
(2020)Doi:10.1081/SCC-120030688
(2004)Doi:10.1021/acs.orglett.8b02793
(2018)