Abstract

Introduction. Currently, more than 600 thousand people a year are affected by malignant tumors on the territory of the Russian Federation. Despite the large selection of antitumor drugs and the variety of mechanisms of their action, the effectiveness of existing drugs continues to be insufficient. The main disadvantages of most antitumor drugs are the emergence of tolerance to them of tumor cells, a limited range of action and high toxicity. In this regard, the creation of effective original domestic antitumor drugs still remains relevant. Among the numerous natural and synthetic heterocyclic compounds that exhibit antitumor activity, indolo[2,3-a]carbazole derivatives that can initiate various pathways of tumor cell death are of increasing interest. The main targets for their action are topoisomerases and protein kinases, which play an important role in the processes of replication, transcription, repair or recombination of deoxyribonucleic acid (DNA). Due to this, in addition to antitumor activity, this group of compounds shows antibacterial, аntiprotozoal and immunomodulatory activity, which makes them a very promising class of candidates for the creation of new drugs.Text. The purpose of this review is to discuss instrumental methods for qualitative and quantitative analysis of indolo[2,3-a]carbazole derivatives used in the world's leading pharmacopoeias. These methods can be used both in pharmacokinetic studies, and in the standardization of these compounds, in the form of pharmaceutical substances, or as part of drug forms.Conclusion. To further introduce a new group of antitumor drugs based on indole[2,3-a]carbazole derivatives into medical practice, a deep and thorough study of their physical and chemical properties is necessary. Justification and development of analysis methods allow us to develop methods applicable to pharmacokinetic studies, as well as to create regulatory documents for quality control and standardization of indolo[2,3-a] carbazole derivatives as pharmaceutical substances. A study of the literature that describes methods for analyzing indolo[2,3-a]carbazole derivatives indicates that spectrometric (infrared and ultraviolet spectrometry) and chromatographic (thin-layer chromatography and high-performance liquid chromatography) methods are most often used to determine the authenticity and quantitative analysis of these compounds.

Highlights

  • More than 600 thousand people a year are affected by malignant tumors on the territory of the Russian Federation

  • Получившее лабораторный шифр UCN-01, обнаруживали в плазме крови и слюне с использованием диодно-матричного детектора, колонки Nova-Pak Phenyl размером 150 × 3,9 мм и подвижной фазы (ПФ), состоящей из 0,05 М раствора аммония ацетата в воде и ацетонитрила

  • Forenza S., Lan Kin S., Matson J

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Summary

СПЕКТРАЛЬНЫЕ МЕТОДЫ АНАЛИЗА

Инфракрасная (ИК-) спектроскопия широко используется при качественной характеристике выделенных из природных источников или синтетических производных индоло[2,3-а]карбазола. Соединение AT2433-A1, выделенное из Actinomadura melliaura (рисунок 3), имеет полосы поглощения с пиками при 3425 и 3362 см-1. Примерами таких соединений являются фториндолокарбазолы B и C (рисунки 6 b, c) с пиками при 1745 см-1 и 1752 см-1 соответственно, которые указывают на наличие малемидной группы в их структуре. Ряд отечественных синтетических производных индоло[2,3-а]карбазола, проявивших противоопухолевую активность, с общей формулой, изображенной на рисунке 6 и лабораторным шифром ЛХС, имеют в ИК-спектре характерные для малемидной группы полосы при 1750, 1730 и 1745 см-1 [18]. Наличие в структуре всех производных индоло[2,3-а]карбазола большого количества сопряженных π-связей позволяет успешно применять метод ультрафиолетовой (УФ-) спектрофотометрии как для идентификации этих соединений, так и для их ко-. Отечественное производное индоло[2,3-а]карбазола ЛХС-1208 имеет максимумы поглощения при 287, 320 и 420 нм в диметилфомамиде. Описанное выше соединение с лабораторным шифром AT2433-A1, демонстрирует максимумы поглощения при 283, 316 и 395 нм с максимальной экстинкцией 45562 при 316 нм [15]

Хроматографические методы анализа
Система растворителей Solvent system

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