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Synthesis and Biological Evaluation of Novel Mono- and Bivalent ASGP-R-targeted Drug-conjugatesстатья
- Авторы: Петров Р.А., Маклакова С.Ю., Иваненков Ю.А., Петров С.А., Сергеева О.В., Ямансаров Е.Ю., Салтыкова И.В., Киреев И.И., Алиева И.Б., Дейнека Е.В., Софронова А.А., Аладинская А.В., Трофименко А.В., Ямиданов Р.С., Ковалев С.В., Котельянский В.Е.
- Журнал: Bioorganic and Medicinal Chemistry Letters
- Год издания: 2017
- Издательство: Pergamon Press Ltd.
- Местоположение издательства: United Kingdom
- DOI: 10.1016/j.bmcl.2017.12.032
- Аннотация: Asialoglycoprotein receptor (ASGP-R) is a promising biological target for drug delivery into hepatoma cells. Nevertheless, there are only few examples of small-molecule conjugates of ASGP-R selective ligand equipped by a therapeutic agent for the treatment of hepatocellular carcinoma (HCC). In the present work, we describe a convenient and versatile synthetic approach to novel mono- and multivalent drug-conjugates containing N-acetyl-2-deoxy-2-aminogalactopyranose and anticancer drug - paclitaxel (PTX). Several molecules have demonstrated high affinity towards ASGP-R and good stability under physiological conditions, significant in vitro anticancer activity comparable to PTX, as well as good internalization via ASGP-R-mediated endocytosis. Therefore, the conjugates with the highest potency can be regarded as a promising therapeutic option against HCC.
- Добавил в систему: Мажуга Александр Георгиевич