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Novel Amide Functionalized Trifluoromethyl thieno[2,3-b]pyridine Derivatives: Anti-cancer Activity and Molecular Docking Studies
Letters in Organic Chemistry ( IF 0.7 ) Pub Date : 2024-01-24 , DOI: 10.2174/0115701786272432231211100408 Sailu Betala 1 , Naveen Puram 1 , Udayasri Bhanothu 1
Letters in Organic Chemistry ( IF 0.7 ) Pub Date : 2024-01-24 , DOI: 10.2174/0115701786272432231211100408 Sailu Betala 1 , Naveen Puram 1 , Udayasri Bhanothu 1
Affiliation
Our primary research objective is to create and formulate small ring heterocycles with enhanced biological efficacy. Amide functionalized trifluoromethyl thieno[2,3-b]pyridine derivatives as a series were prepared starting from reaction between 1,3 di-ketone and thiocyanoacetamide and obtained pyridine 3. Compound 3 reacts with bromoethyl acetate and obtained compound 4, further compound 4 on reaction with diverse substituted aromatic and aliphatic amines to get amide derivatives 5a-d, 6a-d and 7a-h. All the final compounds evaluated for anti cancer activity against four human 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)’ and promising compounds 7d, 7e and 7f have been identified. For compounds 7d, 7e and 7f molecular docking interactions have been identified.
中文翻译:
新型酰胺功能化三氟甲基噻吩并[2,3-b]吡啶衍生物:抗癌活性和分子对接研究
我们的主要研究目标是创造和配制具有增强生物功效的小环杂环。以1,3二酮与硫氰基乙酰胺反应为原料,制备了一系列酰胺官能化的三氟甲基噻吩并[2,3-b]吡啶衍生物,得到吡啶3。化合物3与溴乙酸乙酯反应得到化合物4,进一步得到化合物4。与多种取代的芳香族和脂肪族胺反应得到酰胺衍生物5a-d、6a-d和7a-h。所有最终化合物均针对四种人类癌细胞系(例如“HeLa - 宫颈癌(CCL-2)”)的抗癌活性进行了评估。 COLO 205-结肠癌(CCL-222); HepG2 - 肝癌 (HB-8065); MCF7 - 乳腺癌 (HTB-22)' 和有前景的化合物 7d、7e 和 7f 已被鉴定。对于化合物 7d、7e 和 7f,分子对接相互作用已被鉴定。
更新日期:2024-01-24
中文翻译:
新型酰胺功能化三氟甲基噻吩并[2,3-b]吡啶衍生物:抗癌活性和分子对接研究
我们的主要研究目标是创造和配制具有增强生物功效的小环杂环。以1,3二酮与硫氰基乙酰胺反应为原料,制备了一系列酰胺官能化的三氟甲基噻吩并[2,3-b]吡啶衍生物,得到吡啶3。化合物3与溴乙酸乙酯反应得到化合物4,进一步得到化合物4。与多种取代的芳香族和脂肪族胺反应得到酰胺衍生物5a-d、6a-d和7a-h。所有最终化合物均针对四种人类癌细胞系(例如“HeLa - 宫颈癌(CCL-2)”)的抗癌活性进行了评估。 COLO 205-结肠癌(CCL-222); HepG2 - 肝癌 (HB-8065); MCF7 - 乳腺癌 (HTB-22)' 和有前景的化合物 7d、7e 和 7f 已被鉴定。对于化合物 7d、7e 和 7f,分子对接相互作用已被鉴定。