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探索喹诺酮骨架:解析抗癌药物设计的化学原理。

Exploring Quinolone Scaffold: Unravelling the Chemistry of Anticancer Drug Design.

作者信息

Sharma Vishal, Das Rina, Mehta Dinesh Kumar, Sharma Diksha, Sahu Ram Kumar

机构信息

MM College of Pharmacy, Maharishi Markandeshwar (Deemed to be University), Mullana, Ambala, Hr 133207, India.

Faculty of Pharmaceutical Sciences, Kurukshetra University, Kurukshetra-Hr.

出版信息

Mini Rev Med Chem. 2022;22(1):69-88. doi: 10.2174/1389557521666210112142136.

Abstract

Globally, cancer is considered as the major leading cause in burdening the patient's health care system globally. The growing threat of drug-resistant cancers renders an urgent need to develop more successful candidates for the anti-cancer therapy. In view of the outstanding pharmacological activities, Quinolone and its derivatives have attracted more attention towards drug designing and biological evaluation in the search for new drug molecules. The inspired researchers attempted efforts in order to discover the quinolone based analogs due to their wide range of biological activities. Due to immense pharmacological importance, distinct synthetic methods have been executed to attain new drug entities from quinolones and all the reported molecules have shown constructive anticancer activities. Some of the synthetic protocols like one pot synthesis, post-Ugi-transformation, catalysed based synthesis, enzyme-based synthesis and nano-catalyst based synthetic procedures are also discussed as recent advancements in the production of quinolone derivatives. In this review, recent synthetic approaches in the medicinal chemistry of quinolones and potent quinolone derivatives on the basis of structural activity relationship are outlined. Moreover, their major methods and modifications are discussed.

摘要

在全球范围内,癌症被视为使全球患者医疗保健系统负担加重的主要首要原因。耐药性癌症日益增长的威胁使得迫切需要开发更成功的抗癌治疗候选药物。鉴于喹诺酮及其衍生物出色的药理活性,在寻找新药物分子的过程中,它们在药物设计和生物学评估方面吸引了更多关注。受启发的研究人员努力探索基于喹诺酮的类似物,因为它们具有广泛的生物活性。由于具有巨大的药理重要性,人们已经采用了不同的合成方法来从喹诺酮中获得新的药物实体,并且所有报道的分子都显示出积极的抗癌活性。一些合成方案,如一锅合成、乌吉反应后转化、催化合成、酶促合成和基于纳米催化剂的合成方法,也作为喹诺酮衍生物生产的最新进展进行了讨论。在这篇综述中,概述了喹诺酮药物化学中基于构效关系的最新合成方法以及有效的喹诺酮衍生物。此外,还讨论了它们的主要方法和改进。

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