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Tailoring of novel biologically active molecules based on N-substituted sulfonamides bearing thiazole moiety exhibiting unique multi-addressable biological potentials
Arabian Journal of Chemistry ( IF 5.3 ) Pub Date : 2020-05-01 , DOI: 10.1016/j.arabjc.2020.03.014
Essam M. Hussein , Munirah M. Al-Rooqi , Amal A. Elkhawaga , Saleh A. Ahmed

Abstract Nowadays, the growth of drug-resistant microbial strains (MDRs) is a serious public health threat worldwide. Moreover, tens of millions of people are annually diagnosed with cancer worldwide, and more than half of patients ultimately die. In the present study, a new series of 2-(4-substituted-thiazol-2-ylamino)acetamides and N-(4-substituted-thiazol-2-yl)acetamides incorporating sulfonamide moieties were designed, synthesized, well-characterized and successfully evaluated for their antimicrobial activity against multidrug resistant strains and screened for cytotoxic activity against normal lung fibroblast (WI-38), human lung carcinoma (A549), and human breast carcinoma (MDA-MB-231) cell lines. Fluorescence-activated cell sorting (FACS) analysis and molecular modeling study were performed to identify the mode of action of the novel synthesized compounds and their binding interactions with the active sites of dihydrofolate reductase enzyme (DHFR).

中文翻译:

基于具有噻唑部分的 N 取代磺酰胺的新型生物活性分子的定制,展示独特的多可寻址生物潜力

摘要 如今,耐药微生物菌株(MDRs)的增长是全球严重的公共卫生威胁。此外,全世界每年有数千万人被诊断出患有癌症,超过一半的患者最终死亡。在本研究中,设计、合成了一系列新的 2-(4-取代-噻唑-2-基氨基)乙酰胺和 N-(4-取代-噻唑-2-基)乙酰胺并结合了磺酰胺部分。成功评估了它们对多药耐药菌株的抗菌活性,并筛选了对正常肺成纤维细胞 (WI-38)、人肺癌 (A549) 和人乳腺癌 (MDA-MB-231) 细胞系的细胞毒活性。
更新日期:2020-05-01
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