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Antiproliferative Phenothiazine Hybrids as Novel Apoptosis Inducers against MCF-7 Breast Cancer.

ABSTRACT: 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 ?M. 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.

SUBMITTER: Zhang JX

PROVIDER: S-EPMC6100384 | biostudies-literature | 2018 May

REPOSITORIES: biostudies-literature

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Antiproliferative Phenothiazine Hybrids as Novel Apoptosis Inducers against MCF-7 Breast Cancer.

Zhang Jun-Xia JX Guo Jiao-Mei JM Zhang Ting-Ting TT Lin Hong-Jun HJ Qi Nai-Song NS Li Zhen-Guo ZG Zhou Ji-Chun JC Zhang Zhen-Zhong ZZ

Molecules (Basel, Switzerland) 20180528 6

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 <b>9f</b> showed the most potent inhibitory effect against MCF-7 cells, with an IC<sub>50</sub> va ...[more]

PMID: 29843370

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