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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Indole-fused azepines and analogues as anticancer lead molecules: Privileged findings and future directions
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Indole-fused azepines and analogues as anticancer lead molecules: Privileged findings and future directions

机译:吲哚融合的偶氮病和类似物作为抗癌铅分子:特权调查结果和未来方向

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Abstract The search for new lead compounds of simple structure, displaying highest quality anti-tumor potency with new mechanisms of action and least adverse effects is the major intention of cancer drug discovery now a days. For the time being, indole-fused azepines emerged as a simple class of compounds prolifically designed with strong pharmacological significances in particular of cancer protecting ability. In the recent years from the efforts of our research group, indole-fused heteroazepines, a simple structural class achieved by fusion of indole with oxygen, sulphur and nitrogen containing heteroazepine rings, have known for its superior outcomes in cancer treatment. Surprisingly, the chemistry and biology of these unique families with an amazing role in cancer drug discovery has remained broadly unexplored. This short review is consequently an endeavor to highlight the preliminary ideas over this structural class and to draw the medical attention towards future development of indole-fused azepines and analogues for their promising function in cancer drug discovery. Graphical abstract This review outlines the critical aspects of design and structure-activity relationship (SAR) of indole-fused azepines and related ring-fused systems as anticancer agents with important synthetic strategies. Display Omitted Highlights ? The review gives insights into the current status of indole-fused azepines and analogues. ? The design strategy and SAR are presented in easily understandable graphical manner. ? The review also compiles important synthetic strategies of the present structural scaffold. ? The review highlights the future needs for the development of this structural scaffold.
机译:摘要寻找新的铅化合物的简单结构,呈现最高质量的抗肿瘤效力,具有新的作用机制,最不利影响是癌症药物发现现在的主要意图。暂时,吲哚融合的偶氮病如一种简单的类化合物,这些化合物剧集,癌症保护能力特别具有较强的药理学意义。在近年来,从我们的研究组的努力,吲哚融合异质肽,通过吲哚与含氧,硫和含有含有杂芳酮环的融合来实现的简单结构类,以其癌症治疗的优越结果已知。令人惊讶的是,这些独特的家庭的化学和生物学在癌症药物发现中具有惊人的作用仍然是广泛的未开发的。因此,这段简短的评论因此,努力突出对该结构阶级的初步思想,并在癌症药物发现中为其有希望的功能的吲哚融合的偶氮病和类似物的外观发展的医学关注。图形摘要本综述概述了吲哚融合的偶氮病和相关环形系统的设计和结构 - 活动关系(SAR)作为具有重要合成策略的抗癌剂的关键方面。显示省略亮点?审查提供了对吲哚融合偶氮病和类似物的当前状态的见解。还是设计策略和SAR以易于理解的图形方式呈现。还是审查还汇总了本结构脚手架的重要合成策略。还是审查突出了该结构脚手架的发展未来需求。

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