Novel trifluoromethyl-thieno[2,3-b]pyridine-2-carboxamide and Schiff’s base derivatives and their anticancer activity

Q4 Earth and Planetary Sciences Research Journal of Chemistry and Environment Pub Date : 2023-08-15 DOI:10.25303/2709rjce069074
Balakishan Vadla, Naveen Puram, Sailu Betala
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引用次数: 0

Abstract

A series of novel trifluoromethyl-thieno[2,3-b] pyridine-2-carboxamide 3a-h and Schiff’s base derivatives 5a-g was prepared starting from 6-methyl-2-oxo-4-(trifluoromethyl)-1,2-dihydropyridine-3-carb onitrile 1. Compound 1 on reaction with bromoethyl acetate produced ester derivative 2 on reaction with different amines produced amide derivatives 3. Ester derivative 2 which on reaction with hydrazine hydrate gave hydrazide 4 derivative. Further this compound on reaction with different substituted aromatic aldehydes formed Schiff’s base derivatives 5. All the products 3a-h and 5a-f were screened against four human cancer cell lines such as HeLa -Cervical cancer (CCL-2), COLO 205-Colon cancer (CCL-222), HepG2-Liver cancer (HB-8065) and MCF7-Breast cancer (HTB-22). Promising compounds 3a and 3c have been identified with reference to standard control of 5-Fluorouracil.
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新型三氟甲基噻吩[2,3-b]吡啶-2-羧酰胺和席夫碱衍生物及其抗癌活性
以6-甲基-2-氧-4-(三氟甲基)-1,2-二氢吡啶-3-碳腈1为起始原料,制备了一系列新型三氟甲基噻吩[2,3-b]吡啶-2-羧酰胺3a-h和希夫碱衍生物5a-g。化合物1与溴乙酸乙酯反应生成酯类衍生物2与不同胺反应生成酰胺类衍生物3。酯衍生物2与水合肼反应生成肼衍生物4。此外,该化合物与不同取代芳醛反应形成希夫碱衍生物5。所有产品3a-h和5a-f均对HeLa -宫颈癌(CCL-2)、COLO 205-结肠癌(CCL-222)、hepg2 -肝癌(HB-8065)和mcf7 -乳腺癌(HTB-22) 4种人癌细胞系进行了筛选。参考5-氟尿嘧啶的标准对照,确定了有前途的化合物3a和3c。
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195
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4-8 weeks
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