1393083-39-0Relevant articles and documents
Antiproliferative phenothiazine hybrids as novel apoptosis inducers against MCF-7 breast cancer
Zhang, Jun-Xia,Guo, Jiao-Mei,Zhang, Ting-Ting,Lin, Hong-Jun,Qi, Nai-Song,Li, Zhen-Guo,Zhou, Ji-Chun,Zhang, Zhen-Zhong
, (2018)
We designed a series of novel phenothiazine-1,2,3-triazole hybrids by the molecular hybridization strategy and evaluated their antiproliferative activity against three cancer cell lines (MDA-MB-231, MDA-MB-468 and MCF-7). For the structure-activity relationships, the importance of 1,2,3-triazole and substituents on phenyl ring was explored. Among these phenothiazine-1,2,3-triazole hybrids, compound 9f showed the most potent inhibitory effect against MCF-7 cells, with an IC50 value of 0.8 μM. Importantly, compound 9f could induce apoptosis against MCF-7 cells by regulating apoptosis-related proteins (Bcl-2, Bax, Bad, Parp, and DR5). These potent phenothiazine-1,2,3-triazole hybrids as novel apoptosis inducers might be used as antitumor agents in the future.