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Synthesis of novel aryl and coumarin substituted pyrazolo[1,5-a]pyrimidine derivatives as potent anti-inflammatory and anticancer agents
Chemical Data Collections Pub Date : 2020-12-01 , DOI: 10.1016/j.cdc.2020.100550
Nirmala S. Naik , Lokesh A. Shastri , Bahubali M. Chougala , S. Samundeeswari , Megharaja Holiyachi , Shrinivas D. Joshi , Vinay Sunagar

Abstract Inhibitors of inflammations are considered to be promising compounds in the treatment of cancer associates with inflammations. New Biginelli like targets such as; aryl/coumarin pyrazolo[1,5-a]pyrimidines were accomplished via three component approach. The obtained molecules were assayed for their anti-inflammatory activity by protein denaturation method and the quantitative structure activity relationship (QSAR) results showed remarkable activity at various substitution (R and R') pattern around the aromatic ring (Phenyl/coumarin). While, the antiproliferative activity against different human cell lines showed reduced activity, it might be the low sensitivity of synthesized compounds against cancer cell lines. The docking study was performed with PDB-1BNAand results obtained are significant.

中文翻译:

新型芳基和香豆素取代的吡唑并[1,5-a]嘧啶衍生物的合成作为有效的抗炎和抗癌剂

摘要 炎症抑制剂被认为是治疗与炎症相关的癌症的有前途的化合物。新的 Biginelli 喜欢目标,例如;芳基/香豆素吡唑并[1,5-a]嘧啶是通过三组分方法完成的。通过蛋白质变性方法测定所得分子的抗炎活性,定量结构活性关系(QSAR)结果显示在芳环(苯基/香豆素)周围的各种取代(R和R')模式下具有显着的活性。虽然对不同人类细胞系的抗增殖活性显示出降低的活性,但可能是合成化合物对癌细胞系的敏感性低。对接研究是用PDB-1BNA进行的,获得的结果是显着的。
更新日期:2020-12-01
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