新型1,2,3-三唑标记的吡唑并[3,4-b]吡啶衍生物的合成及其细胞毒性活性。
Synthesis of novel 1,2,3-triazole tagged pyrazolo[3,4-b]pyridine derivatives and their cytotoxic activity.
作者信息
Kurumurthy Chavva, Veeraswamy Banda, Sambasiva Rao Pillalamarri, Santhosh Kumar Gautham, Shanthan Rao Pamulaparthy, Loka Reddy Velaturu, Venkateswara Rao Janapala, Narsaiah Banda
机构信息
Fluoro Organic Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 607, India.
Biology division, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500 607, India.
出版信息
Bioorg Med Chem Lett. 2014 Feb 1;24(3):746-9. doi: 10.1016/j.bmcl.2013.12.107. Epub 2014 Jan 3.
A series of novel 1,2,3-triazole tagged pyrazolo[3,4-b]pyridine derivatives 3 and 4 were prepared respectively starting from 6-phenyl-4-(trifluoromethyl)-1H-pyrazolo[3,4-b]pyridin-3-amine 1 via selective N-propargylation, followed by reaction with diverse substituted alkyl/perfluoroalkyl/aryl/aryl amide azides under Sharpless conditions. All the synthesized compounds 3 and 4 were screened for cytotoxic activity against four human cancer cell lines such as U937, THP-1, HL60 and B16-F10. Compounds 3e, 4g, 4i and 4j which showed promising activity have been identified.
分别从6-苯基-4-(三氟甲基)-1H-吡唑并[3,4-b]吡啶-3-胺1开始，通过选择性N-炔丙基化反应，制备了一系列新型的带有1,2,3-三唑标记的吡唑并[3,4-b]吡啶衍生物3和4，随后在Sharpless条件下与各种取代的烷基/全氟烷基/芳基/芳基酰胺叠氮化物反应。对所有合成的化合物3和4针对四种人类癌细胞系（如U937、THP-1、HL60和B16-F10）进行了细胞毒性活性筛选。已鉴定出显示出有前景活性的化合物3e、4g、4i和4j。
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