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Synthesis of novel isoxazole functionalized pyrazolo[3,4‐b]pyridine derivatives; their anticancer activity
Journal of Heterocyclic Chemistry ( IF 2.4 ) Pub Date : 2020-05-08 , DOI: 10.1002/jhet.3968
Sampath Ravula 1 , Ramana Reddy Bobbala 1 , Balakrishna Kolli 1
Affiliation  

A series of novel isoxazole functionalized pyrazolo[3,4‐b]pyridine derivatives 5a‐n were prepared, respectively, initiated from 6‐thiophenyl‐4‐(trifluoromethyl)‐1H ‐pyrazolo[3,4‐b ]pyridin‐3‐amine 3 through selective N ‐propargylation, and these N ‐propargylated compounds 4 were cyclized with aryloximes by using of sodium hypochlorite, and obtained the title products 5a‐n . All the final products 5a‐n were submitted for anticancer activity against four cancer cell lines such as “HeLa—cervical cancer (CCL‐2); COLO 205—colon cancer (CCL‐222); HepG2—liver cancer (HB‐8065); MCF7—breast cancer (HTB‐22)”; Compounds 5c , 5d , and 5h are found to have more prominent anticancer activity at micro molar concentration.

中文翻译:

新型异恶唑官能化的吡唑并[3,4-b]吡啶衍生物的合成;他们的抗癌活性

一系列新颖的异恶唑官能吡唑并[3,4-b]吡啶衍生物的图5a-n的制备,分别从6-噻吩基-4-(三氟甲基)-1发起ħ -吡唑并[3,4- b ]吡啶-3-胺3通过选择性N炔丙基化,而这些N炔丙基化的化合物4通过使用次氯酸钠与芳肟环合,获得标题产物5a-n。所有最终产品5a‐n已提交针对四种癌细胞系(例如“ HeLa-宫颈癌(CCL-2)”)的抗癌活性;COLO 205-结肠癌(CCL‐222);HepG2-肝癌(HB-8065);MCF7-乳腺癌(HTB-22)”;发现化合物5c5d5h在微摩尔浓度下具有更突出的抗癌活性。
更新日期:2020-05-08
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