ANTITUMOR DRUGS BASED ON INDOLOCARBAZOL DERIVATIVES

I. P. Kolpaksidi, M. Dmitrieva, I. V. Yarosh, I. Krasnyuk
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引用次数: 1

Abstract

The aim of the work is to generalize the literature data on indolocarbazole derivatives with an antitumor activity.Materials and methods. The objects of the study were the preparations based on indolocarbazole derivatives with the antitumor activity. To search for materials on the problem under study, the following search and information as well as library databases were used: ebibrary, PubMed, CyberLeninka, ResearchGate, the State Register of Medicines, clinical trials registries clinline.ru and clinicaltrials.gov. The search for the following words / phrases was performed: indolocarbazoles, indolocarbazole derivatives, staurosporine, rebeccamycin, staurosporine derivatives. The search was conducted from January 11 until March 1, 2021. The compounds with a biological activity which were undergoing or had undergone preclinical and clinical trials, were taken into account. All the materials from 1977 to January 1, 2021, were taken into account.Results. The materials obtained indicate that indolocarbazole derivatives are promising compounds for the creation of anticancer medicinal preparations due to their properties and peculiarities of the action mechanism. These drugs have a selective action due to the targeted interaction with specific molecular targets: kinases (especially protein kinase C and its isozymes), DNA and DNA topoisomerase. To date, many compounds from the class of indolocarbazoles have been synthesized and investigated. They have shown a high antitumor activity in the treatment of systemic and solid tumors. However, despite this, only one MP based on a staurosporine derivative, registered by the TN of Rydapt® (in the USA and EU countries) and Miticaid® (in the Russian Federation), is approved for use in the clinical practice.Conclusion. Thus, the basic data from scientific publications on promising anticancer medicinal preparations based on compounds from the class of indolocarbazoles, have been summarized. The information is provided, in particular, on their molecular structure, the origin, classification, the main representatives of the class, which are at various stages of the research and are approved for use in the clinic.
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基于吲哚咔唑衍生物的抗肿瘤药物
本工作的目的是总结具有抗肿瘤活性的吲哚咔唑衍生物的文献资料。材料和方法。以吲哚咔唑衍生物为基础,研究具有抗肿瘤活性的制剂。为了搜索研究中问题的资料,使用了以下搜索和信息以及图书馆数据库:elibrary、PubMed、CyberLeninka、ResearchGate、国家药品注册、临床试验注册clinine .ru和clinicaltrials.gov。查询的单词/短语为:吲哚咔唑,吲哚咔唑衍生物,staurosporine, rebecycin, stausporine衍生物。搜寻工作从1月11日持续到2021年3月1日。正在进行或已经进行临床前和临床试验的具有生物活性的化合物被考虑在内。选取了1977年至2021年1月1日的所有资料。所获得的材料表明,吲哚咔唑衍生物由于其性质和作用机制的特殊性,是有前景的抗癌药物制剂的化合物。这些药物由于与特定分子靶标的靶向相互作用而具有选择性作用:激酶(特别是蛋白激酶C及其同工酶)、DNA和DNA拓扑异构酶。迄今为止,已经合成和研究了吲哚咔唑类的许多化合物。它们在治疗全身和实体肿瘤中显示出很高的抗肿瘤活性。然而,尽管如此,只有一种基于staurosporine衍生物的MP,由rydap®(在美国和欧盟国家)和Miticaid®(在俄罗斯联邦)的TN注册,被批准用于临床实践。因此,从科学出版物的基本数据总结了基于吲哚咔唑类化合物的有前途的抗癌药物制剂。提供的信息,特别是关于它们的分子结构,起源,分类,该类的主要代表,它们处于研究的不同阶段,并被批准用于临床。
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