Synthesis of 3-phenylpyrazolopyrimidine-1,2,3-triazole conjugates and evaluation of their Src kinase inhibitory and anticancer activities

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:21

Article

Kumar, Anil^1,2  Ahmad, Israr¹  Chhikara, Bhupender S.²  Tiwari, Rakesh²  Mandal, Deendayal²  Parang, Keykavous² 

[1] Birla Inst Technol & Sci, Dept Chem, Pilani 333031, Rajasthan, India

[2] Univ Rhode Isl, Dept Biomed & Pharmaceut Sci, Kingston, RI 02881 USA

关键词: Anticancer activity;    Click reaction;    Phenylpyrazolopyrimidine;    Src kinase;    1,2,3-Triazole;    Tyrosine kinase;   

DOI  :  10.1016/j.bmcl.2011.01.047

来源: Elsevier

【 摘 要 】

A series of two classes of 3-phenylpyrazolopyrimidine-1,2,3-triazole conjugates were synthesized using click chemistry approach. All compounds were evaluated for inhibition of Src kinase and human ovarian adenocarcinoma (SK-Ov-3), breast carcinoma (MDA-MB-361), and colon adenocarcinoma (HT-29). Hexyl triazolyl-substituted 3-phenylpyrazolopyrimidine exhibited inhibition of Src kinase with an IC50 value of 5.6 mu M. 4-Methoxyphenyl triazolyl-substituted 3-phenylpyrazolopyrimidine inhibited the cell proliferation of HT-29 and SK-Ov-3 by 73% and 58%, respectively, at a concentration of 50 mu M. (C) 2011 Elsevier Ltd. All rights reserved.

【 授权许可】

Free