新型酰胺官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

IF 0.7 4区 化学 Q4 CHEMISTRY, ORGANIC Letters in Organic Chemistry Pub Date : 2024-01-26 DOI:10.2174/0115701786272432231211100408
Sailu Betala, Naveen Puram, Udayasri Bhanothu
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引用次数: 0

摘要

:我们的主要研究目标是创造和配制具有更强生物功效的小环杂环。从 1,3 二酮与硫氰基乙酰胺反应得到吡啶 3 开始,制备了酰胺官能化三氟甲基噻吩并[2,3-b]吡啶衍生物系列。化合物 3 与溴乙酸乙酯反应,得到化合物 4,化合物 4 再与各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。对所有最终化合物针对四种人类癌细胞系(如 HeLa - 宫颈癌 (CCL-2);COLO 205 - 结肠癌 (CCL-222);HepG2 - 肝癌 (HB-8065);MCF7 - 乳腺癌 (HTB-22))的抗癌活性进行了评估,并确定了有前景的化合物 7d、7e 和 7f。化合物 7d、7e 和 7f 的分子对接相互作用已经确定:合成结果:我们合成了酰胺官能化的噻吩并吡啶酮衍生物,并评估了四种人类癌症细胞系的抗癌活性
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Novel Amide Functionalized Trifluoromethyl thieno[2,3-b]pyridine Derivatives: Anti-cancer Activity and Molecular Docking Studies
: 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. background: heterocyclic chemistry method: Synthesis result: we synthesized amide functionalized thienopyridone derivates and evaluated for anticancer activity four human cancer cell lines
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来源期刊
Letters in Organic Chemistry
Letters in Organic Chemistry 化学-有机化学
CiteScore
1.30
自引率
12.50%
发文量
135
审稿时长
7 months
期刊介绍: Aims & Scope Letters in Organic Chemistry publishes original letters (short articles), research articles, mini-reviews and thematic issues based on mini-reviews and short articles, in all areas of organic chemistry including synthesis, bioorganic, medicinal, natural products, organometallic, supramolecular, molecular recognition and physical organic chemistry. The emphasis is to publish quality papers rapidly by taking full advantage of latest technology for both submission and review of the manuscripts. The journal is an essential reading for all organic chemists belonging to both academia and industry.
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