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Targeted 1,3-dipolar cycloaddition with acrolein for cancer prodrug activation

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dc.contributor.author Pradipta A.R.
dc.contributor.author Ahmadi P.
dc.contributor.author Terashima K.
dc.contributor.author Muguruma K.
dc.contributor.author Fujii M.
dc.contributor.author Ichino T.
dc.contributor.author Maeda S.
dc.contributor.author Tanaka K.
dc.date.accessioned 2022-02-09T20:46:42Z
dc.date.available 2022-02-09T20:46:42Z
dc.date.issued 2021
dc.identifier.issn 2041-6520
dc.identifier.uri https://dspace.kpfu.ru/xmlui/handle/net/170216
dc.description.abstract Cytotoxic anticancer drugs used in chemotherapy are often antiproliferative agents that preferentially kill rapidly growing cancer cells. Their mechanism relies mainly on the enhanced proliferation rate of cancer cells and is not genuinely selective for cancer cells. Therefore, these drugs can also significantly affect healthy cells. Prodrug therapy provides an alternative approach using a less cytotoxic form of anticancer drug. It involves the synthesis of inactive drug derivatives which are converted to an active form inside the body and, preferably, only at the site of cancerous tissues, thereby reducing adverse drug reaction (ADR) events. Herein, we demonstrate a prodrug activation strategy by utilizing the reaction between aryl azide and endogenous acrolein. Since acrolein is generally overproduced by most cancer cells, we anticipate our strategy as a starting point for further applications in mouse models with various cancers. Furthermore, cancer drugs that have had therapeutic index challenges might be reconsidered for application by utilizing our strategy.
dc.relation.ispartofseries Chemical Science
dc.title Targeted 1,3-dipolar cycloaddition with acrolein for cancer prodrug activation
dc.type Article
dc.relation.ispartofseries-issue 15
dc.relation.ispartofseries-volume 12
dc.collection Публикации сотрудников КФУ
dc.relation.startpage 5438
dc.source.id SCOPUS20416520-2021-12-15-SID85104831295


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  • Публикации сотрудников КФУ Scopus [24551]
    Коллекция содержит публикации сотрудников Казанского федерального (до 2010 года Казанского государственного) университета, проиндексированные в БД Scopus, начиная с 1970г.

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