Literature DB >> 25655718

Design and synthesis of novel 1,2,3-triazole-pyrimidine-urea hybrids as potential anticancer agents.

Li-Ying Ma1, Bo Wang1, Lu-Ping Pang1, Miao Zhang1, Sai-Qi Wang1, Yi-Chao Zheng1, Kun-Peng Shao1, Deng-Qi Xue1, Hong-Min Liu2.   

Abstract

A series of novel 1,2,3-triazole-pyrimidine-urea hybrids were designed, synthesized and evaluated for anticancer activity against four selected cancer cell lines (MGC-803, EC-109, MCF-7 and B16-F10). Majority of the synthesized compounds exhibited moderate to potent activity against all the cancer cell lines assayed. Particularly, compounds 26, 30 and 38 exhibited excellent growth inhibition against B16-F10 with IC50 values of 32nM, 35nM and 42nM, respectively. Flow cytometry analysis demonstrated that compound 26 induced the cellular apoptosis in a concentration-dependent manner.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Anticancer; Apoptosis; Pyrimidine; Triazole; Urea

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Year:  2015        PMID: 25655718     DOI: 10.1016/j.bmcl.2014.12.087

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  New ursolic acid derivatives bearing 1,2,3-triazole moieties: design, synthesis and anti-inflammatory activity in vitro and in vivo.

Authors:  Tian-Yi Zhang; Chun-Shi Li; Li-Ting Cao; Xue-Qian Bai; Dong-Hai Zhao; Si-Mei Sun
Journal:  Mol Divers       Date:  2021-06-02       Impact factor: 2.943

Review 2.  CuAAC-ensembled 1,2,3-triazole-linked isosteres as pharmacophores in drug discovery: review.

Authors:  Alisha Rani; Gurjaspreet Singh; Akshpreet Singh; Ubair Maqbool; Gurpreet Kaur; Jandeep Singh
Journal:  RSC Adv       Date:  2020-02-04       Impact factor: 4.036

  2 in total

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