Synthesis and anticancer activity evaluation of novel azacalix[2]arene[2]pyrimidines

Eur J Med Chem. 2018 May 10:151:214-225. doi: 10.1016/j.ejmech.2018.02.079.

Yesu Addepalli ¹, Xiaohong Yang ¹, Minghui Zhou ¹, D Prabhakar Reddy ¹, Shao-Lin Zhang ¹, Zhen Wang ², Yun He ³

Affiliations

1 School of Pharmaceutical Sciences and Chongqing Key Laboratory of Natural Drug Research, Chongqing University, 55 Daxuecheng South Road, Shapingba, Chongqing 401331, PR China.
2 School of Pharmaceutical Sciences and Chongqing Key Laboratory of Natural Drug Research, Chongqing University, 55 Daxuecheng South Road, Shapingba, Chongqing 401331, PR China. Electronic address: wangz1114@cqu.edu.cn.
3 School of Pharmaceutical Sciences and Chongqing Key Laboratory of Natural Drug Research, Chongqing University, 55 Daxuecheng South Road, Shapingba, Chongqing 401331, PR China. Electronic address: yun.he@cqu.edu.cn.

PMID: 29614418 DOI: 10.1016/j.ejmech.2018.02.079

Abstract

A series of novel azacalix[2]arene[2]pyrimidines were synthesized, and evaluated for their antiproliferative activities against A549, MCF7, SH-SY5Y and CNE human Cancer cell lines in vitro by using the CCK-8 assay. A number of compounds showed low micromolar antiproliferative activities against MCF7 cell line. Compound 4j, containing a pyrrolidine moiety, exhibited the strongest inhibitory activity with an IC₅₀ value of 0.58 μM. Furthermore, breast Cancer cells were used to explore the inhibition mechanism of these azacalix[2]arene[2]pyrimidines. The results suggested these compounds were involved in inducing cell Apoptosis via up-regulation of Caspase-3 and caspase-9 protein expression, and the cell cycle was arrested at the S phase. Our reports here represent the first studies on the biological activities of azacalix[2]arene[2]pyrimidines.

Keywords

2,4-diaminopyrimidine; Anticancer activity; Antiproliferation; Azacalix[2]arene[2]pyrimidines; Calixarene.

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