Design and synthesis of novel pyrazolo[1,5-a]pyrimidine derivatives bearing nitrogen mustard moiety and evaluation of their antitumor activity in vitro and in vivo

Eur J Med Chem. 2016 Aug 25:119:183-96. doi: 10.1016/j.ejmech.2016.04.068.

Mingxia Zhao ¹, Hongyu Ren ¹, Jin Chang ¹, Diqin Zhang ¹, Yating Yang ¹, Yong He ², Chuanmin Qi ³, Huabei Zhang ¹

Affiliations

1 Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China.
2 Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China; Experimental Chemistry Center, Beijing Normal University, Beijing 100875, PR China.
3 Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China. Electronic address: qicmin@sohu.com.

PMID: 27162123 DOI: 10.1016/j.ejmech.2016.04.068

Abstract

A series of novel pyrazolo[1,5-a]pyrimidine derivatives bearing nitrogen mustard moiety were designed, synthesized and evaluated for their antiproliferative activities against five human Cancer cell lines (A549, SH-SY5Y, HepG2, MCF-7 and DU145) in vitro. Among these compounds, 13b exhibited potent inhibitory effect on the proliferation of the five tumor cells and was able to inhibit cell cycle arrest at G1 phase and induce cell Apoptosis. In HepG2 HCC xenograft compound 13b was selected for evaluating the antitumor activity in vivo which exhibited significant Cancer growth inhibition with low host toxicity in vivo.

Keywords

Anti-tumor; Apoptosis; Cell cycle; Nitrogen mustard derivatives; Pyrazolo[1,5-a]pyrimidine; Xenograft mice model.

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