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Design, Synthesis, and Dual Evaluation of Quinoline and Quinolinium Iodide Salt Derivatives as Potential Anticancer and Antibacterial Agents.
ChemMedChem ( IF 3.6 ) Pub Date : 2020-02-18 , DOI: 10.1002/cmdc.202000002 Guofan Jin 1 , Fuyan Xiao 1 , Zhenwang Li 2 , Xueyong Qi 1 , Lei Zhao 3 , Xianyu Sun 2
ChemMedChem ( IF 3.6 ) Pub Date : 2020-02-18 , DOI: 10.1002/cmdc.202000002 Guofan Jin 1 , Fuyan Xiao 1 , Zhenwang Li 2 , Xueyong Qi 1 , Lei Zhao 3 , Xianyu Sun 2
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A series of novel quinoline and quinolinium iodide derivatives were designed and synthesized to discover potential anticancer and antibacterial agents. With regard to anticancer properties, in vitro cytotoxicities against three human cancer cell lines (A-549, HeLa and SGC-7901) were evaluated. The antibacterial properties against two strains, Escherichia coli (ATCC 29213) and Staphylococcus aureus (ATCC 8739), along with minimum inhibitory concentration (MIC) values were evaluated. The target alkyliodine substituted compounds exhibited significant antitumor and antibacterial activity, of which compound 8-((4-(benzyloxy)phenyl)amino)-7-(ethoxycarbonyl)-5-propyl-[1,3]dioxolo[4,5-g]quinolin-5-ium (12) was found to be the most potent derivative with IC50 values of 4.45±0.88, 4.74±0.42, 14.54±1.96, and 32.12±3.66 against A-549, HeLa, SGC-7901, and L-02 cells, respectively, stronger than the positive controls 5-FU and MTX. Furthermore, compound 12 had the most potent bacterial inhibitory activity. The MIC of this compound against both E. coli and S. aureus was 3.125 nmol ⋅ mL-1 , which was smaller than that against the reference agents amoxicillin and ciprofloxacin.
中文翻译：
设计，合成和双重评估喹啉和喹啉碘化物盐衍生物作为潜在的抗癌和抗菌剂。
设计并合成了一系列新型的喹啉和碘化喹啉鎓衍生物，以发现潜在的抗癌和抗菌剂。关于抗癌特性，评估了对三种人类癌细胞系（A-549，HeLa和SGC-7901）的体外细胞毒性。评估了对两种菌株大肠杆菌（ATCC 29213）和金黄色葡萄球菌（ATCC 8739）的抗菌性能，以及最低抑菌浓度（MIC）值。目标烷基碘取代的化合物表现出显着的抗肿瘤和抗菌活性，其中化合物8-（（4-（苄氧基）苯基）氨基）-7-（乙氧羰基）-5-丙基-[1,3] dioxolo [4,5- g]喹啉-5-鎓（12）被发现是对A-549，HeLa，SGC-7901，IC50值分别为4.45±0.88、4.74±0.42、14.54±1.96和32.12±3.66的最有效衍生物。和L-02细胞分别强于阳性对照5-FU和MTX。此外，化合物12具有最有效的细菌抑制活性。该化合物对大肠杆菌和金黄色葡萄球菌的MIC为3.125 nmol·mL-1，比对参比药物阿莫西林和环丙沙星的MIC小。
更新日期：2020-03-02
中文翻译：
设计，合成和双重评估喹啉和喹啉碘化物盐衍生物作为潜在的抗癌和抗菌剂。
设计并合成了一系列新型的喹啉和碘化喹啉鎓衍生物，以发现潜在的抗癌和抗菌剂。关于抗癌特性，评估了对三种人类癌细胞系（A-549，HeLa和SGC-7901）的体外细胞毒性。评估了对两种菌株大肠杆菌（ATCC 29213）和金黄色葡萄球菌（ATCC 8739）的抗菌性能，以及最低抑菌浓度（MIC）值。目标烷基碘取代的化合物表现出显着的抗肿瘤和抗菌活性，其中化合物8-（（4-（苄氧基）苯基）氨基）-7-（乙氧羰基）-5-丙基-[1,3] dioxolo [4,5- g]喹啉-5-鎓（12）被发现是对A-549，HeLa，SGC-7901，IC50值分别为4.45±0.88、4.74±0.42、14.54±1.96和32.12±3.66的最有效衍生物。和L-02细胞分别强于阳性对照5-FU和MTX。此外，化合物12具有最有效的细菌抑制活性。该化合物对大肠杆菌和金黄色葡萄球菌的MIC为3.125 nmol·mL-1，比对参比药物阿莫西林和环丙沙星的MIC小。
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