Molecules, Vol. 23, Pages 1288: Antiproliferative Phenothiazine Hybrids as Novel Apoptosis Inducers against MCF-7 Breast Cancer

Molecules, Vol. 23, Pages 1288: Antiproliferative Phenothiazine Hybrids as Novel Apoptosis Inducers against MCF-7 Breast Cancer Molecules doi: 10.3390/molecules23061288 Authors: Jun-Xia Zhang Jiao-Mei Guo Ting-Ting Zhang Hong-Jun Lin Nai-Song Qi Zhen-Guo Li Ji-Chun Zhou Zhen-Zhong Zhang 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.
Source: Molecules - Category: Chemistry Authors: Tags: Article Source Type: research