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Eur J Med Chem. 2013 Nov;69:323-30. doi: 10.1016/j.ejmech.2013.08.029. Epub 2013 Sep 4.

A novel [1,2,4] triazolo [1,5-a] pyrimidine-based phenyl-linked steroid dimer: synthesis and its cytotoxic activity.

Author information

1
School of Pharmaceutical Sciences and New Drug Research & Development Center, Zhengzhou University, Zhengzhou 450001, PR China.

Abstract

A novel [1,2,4] triazolo [1,5-a] pyrimidine-based phenyl-linked steroid dimer was designed, synthesized and evaluated for its cytotoxic activity against five human cancer cell lines and the cytotoxicity against human normal liver cell L-02. Compound 3 showed excellent cytotoxic activity and good selectivity between cancer and normal cells. Further mechanistic studies revealed that treatment of EC109 cells with compound 3 caused an obvious G2/M arrest in a concentration- and time-dependent manner and induced apoptosis probably through the mitochondrial pathway accompanied with the decrease of mitochondrial membrane potential, activations of caspase-9/-3, cleavage of MDM2 as well as up-regulation of the expressions of p53 and Bax.

KEYWORDS:

Apoptosis; Cell cycle arrest; Cytotoxicity; Mitochondrial pathway; Steroid dimer; [1,2,4] Triazolo [1,5-a] pyrimidine

PMID:
24077182
DOI:
10.1016/j.ejmech.2013.08.029
[Indexed for MEDLINE]
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