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.
Highlights
Cancer is often referred to as “the pathology of the century” in the context of an endemic disease spreading throughout the world
The article is a review of the publications devoted to indolocarbazole derivatives, i.e., to the information on their structure, origin, classification, the main representatives of the class, which are at various stages of research and are approved for use in the clinic
Indolocarbazole derivatives are a promising class of anticancer drugs characterized by a directed mechanism of the action on targets such as kinases, DNA and DNA topoisomerases I and II
Summary
Cancer is often referred to as “the pathology of the century” in the context of an endemic disease spreading throughout the world. Cancer has been identified as “a true disease of modernity” (Roy Porter) or even “an important product of modernity” (Siddhartha Mukherjee). These two definitions are generally accepted and justified by a sharp increase in morbidity and mortality, which has been observed since the end of the 18th century [1]. In 2020, cancer continued to be one of the leading causes of death and an important obstacle to increasing life expectancy in all countries of the world. Among a wide range of anticancer drugs, compounds from the group of indolocarbazole derivatives are of particular interest. Indolocarbazoles are a unique class of indole alkaloids of a natural or synthetic kinds of origin, which have a number of therapeutic properties
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