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合成 3-苯基吡唑并嘧啶-1,2,3-三唑缀合物，并评价其Src 激酶抑制和抗癌活性。

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

机构信息

Department of Chemistry, Birla Institute of Technology and Science, Pilani, Rajasthan, India.

出版信息

Bioorg Med Chem Lett. 2011 Mar 1;21(5):1342-6. doi: 10.1016/j.bmcl.2011.01.047. Epub 2011 Jan 15.

DOI:10.1016/j.bmcl.2011.01.047
PMID:21300544
Abstract

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 IC(50) value of 5.6 μM. 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 μM.

摘要

采用点击化学方法合成了一系列两类 3-苯基吡唑并嘧啶-1,2,3-三唑共轭物。所有化合物均进行了Src 激酶抑制作用评价和人卵巢腺癌 (SK-Ov-3)、乳腺癌 (MDA-MB-361) 和结肠腺癌 (HT-29) 的细胞增殖抑制活性评价。己基三唑取代的 3-苯基吡唑并嘧啶对 Src 激酶的抑制作用的 IC50 值为 5.6 μM。4-甲氧基苯基三唑取代的 3-苯基吡唑并嘧啶在 50 μM 浓度下分别对 HT-29 和 SK-Ov-3 的细胞增殖抑制率达到 73%和 58%。

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