Recent Overview on the Molecular Hybrids Integrated With Benzosuberone/Benzo[7]annulene Derivatives as Multi-Target Therapeutics

IF 3.5 3区 医学 Q2 CHEMISTRY, MEDICINAL
Mohamed S. Nafie, Kamal M. Dawood, Mohamed K. Diab, Ashraf A. Abbas
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引用次数: 0

Abstract

Benzosuberone is a promising scaffold with a remarkably varied pharmacological profile that has been attracting significant interest in the potential development of anticancer agents. This review focuses on the historical interest, diversity of chemical structures, and different medicinal applications of benzosuberone derivatives, particularly as agents with potential anticancer activity. We investigated the relationship between structure modification and biological activity by focusing on the molecular hybrids of the present hit with various functionalities or heterocycles, which led to improved cytotoxicity against several cancer cell lines, and miscellaneous biological activities such as antimicrobial, antiviral, neurological, antiparasitic, anti-diabetic, and antitubercular activities. Detailed in vitro analyses showed promising cytotoxicity against breast, lung, and colon cancers, presenting IC50 values in the low micromolar and submicromolar ranges and low toxicity profiles concerning normal cells. Novel approaches, including the hybrid molecule, combinatory therapy, and nano-formulation, are suggested to go beyond the current obstacles and expand the applications of benzosuberone-based derivatives toward clinical applications. This combined study demonstrates that the benzosuberone scaffold is a privileged structure in the search for miscellaneous biological drugs with high therapeutic potential.

结合苯并酮/苯并[7]环烯衍生物的分子杂合体多靶点治疗研究进展
苯甲醌是一种很有前途的支架,具有显著不同的药理特征,已经引起了人们对抗癌药物潜在开发的极大兴趣。本文综述了苯并甲酮衍生物的历史意义、化学结构的多样性和不同的医学应用,特别是作为具有潜在抗癌活性的药物。我们研究了结构修饰与生物活性之间的关系,重点研究了具有不同功能或杂环的分子杂种,这些杂种杂种可以提高对几种癌细胞的细胞毒性,以及其他生物活性,如抗菌、抗病毒、神经学、抗寄生虫、抗糖尿病和抗结核活性。详细的体外分析显示,对乳腺癌、肺癌和结肠癌有良好的细胞毒性,在低微磨牙和亚微磨牙范围内显示IC50值,对正常细胞的毒性较低。本文提出了新的途径,包括分子杂交、联合治疗和纳米配方,以突破目前的障碍,扩大苯甲砜类衍生物的临床应用。这一综合研究表明,苯并醌支架是寻找具有高治疗潜力的杂类生物药物的特权结构。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Archiv der Pharmazie
Archiv der Pharmazie 医学-化学综合
CiteScore
7.90
自引率
5.90%
发文量
176
审稿时长
3.0 months
期刊介绍: Archiv der Pharmazie - Chemistry in Life Sciences is an international journal devoted to research and development in all fields of pharmaceutical and medicinal chemistry. Emphasis is put on papers combining synthetic organic chemistry, structural biology, molecular modelling, bioorganic chemistry, natural products chemistry, biochemistry or analytical methods with pharmaceutical or medicinal aspects such as biological activity. The focus of this journal is put on original research papers, but other scientifically valuable contributions (e.g. reviews, minireviews, highlights, symposia contributions, discussions, and essays) are also welcome.
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