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Quinolines, a perpetual, multipurpose scaffold in medicinal chemistry
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2021-01-08 , DOI: 10.1016/j.bioorg.2021.104639
Pratibha Yadav 1 , Kamal Shah 1
Affiliation  

Quinoline is a versatile pharmacophore, a privileged scaffold and an outstanding fused heterocyclic compound with a wide range of pharmacological prospective such as anticancer, anti-inflammatory, antibacterial, antiviral drug and superlative moiety in drug discovery. The quinoline hybrids have already been shown excellent results with new targets with a different mode of actions as an inhibitor of cell proliferation by cell cycle arrest, apoptosis, angiogenesis, disruption of cell migration and modulation. This review emphasized the mode of action, structure activity relationship and molecular docking to reveal the various active pharmacophores of quinoline hybrids accountable for novel anticancer, anti-inflammatory, antibacterial and miscellaneous activities. Therefore, several quinoline candidates are under clinical trials for the treatment of certain diseases, for example ferroquine (antimalarial), dactolisib (antitumor) and pelitinib (EGFR TK inhibitors) etc. Plenty of research has been summarized the recent advances of quinoline derivatives and explore the various therapeutic prospects of this moiety. This review would help the researchers to strategically design diverse novel quinoline derivatives for the development of clinically viable drug candidates for the treatment of incurable diseases.



中文翻译:

喹啉,一种永久的、多用途的药物化学支架

喹啉是一种多功能的药效团、一种特殊的支架和一种杰出的稠合杂环化合物,具有广泛的药理学前景,如抗癌、抗炎、抗菌、抗病毒药物和药物发现中的最高级部分。喹啉杂化物已经显示出优异的结果,新靶点具有不同的作用模式,可通过细胞周期停滞、细胞凋亡、血管生成、细胞迁移和调节的破坏来抑制细胞增殖。这篇综述强调了作用方式、结构活性关系和分子对接,以揭示喹啉杂化物的各种活性药效团,这些药效团负责新的抗癌、抗炎、抗菌和其他活性。所以,几种喹啉候选药物正在进行临床试验,用于治疗某些疾病,例如亚铁喹(抗疟药)、dactolisib(抗肿瘤药)和佩利替尼(EGFR TK 抑制剂)等。大量研究总结了喹啉衍生物的最新进展并探索了各种该部分的治疗前景。该综述将帮助研究人员战略性地设计多种新型喹啉衍生物,以开发临床上可行的候选药物,用于治疗不治之症。

更新日期:2021-01-10
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