A novel pyrazolone-based copper complex [CuL(phen)(CHOH)][CuL(phen)]·CHCHOH·CHOH (P-FAH-Cu-phen) was synthesized and characterized. The asymmetric structural unit of P-FAH-Cu-phen was composed of two independent complex units [CuL(phen)(CHOH)] and [CuL(phen)]:Cu1 center with six coordination mode and Cu2 center with five coordination mode. The growth of BEL-7404 cells and H22 cells was significantly inhibited by P-FAH-Cu-phen with IC values of 1.175 μg/mL and 1.097 μg/mL, respectively, which were much lower than IC of cisplatin for BEL-7404 cells (23.32 μg/mL) and H22 cells (27.5 μg/mL). P-FAH-Cu-phen induced cell cycle arrest at G2/M and apoptosis in BEL-7404 cells through mitochondria- and endoplasmic reticulum stress-associated pathways. Moreover, P-FAH-Cu-phen significantly suppressed the migration of BEL-7404 cells and the tumor growth in H22 tumor mouse model without severe side effects and improved the survival of tumor mice. The results suggested that P-FAH-Cu-phen might be a potential drug candidate for the treatment of live cancer.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7957940 | PMC |
| http://dx.doi.org/10.1021/acsmedchemlett.0c00680 | DOI Listing |
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