Recent Advances in the Synthesis of Polyamine Derivatives and Their Applications

Biogenic polyamines (PAs) are involved in the growth and development of normal cells, and their intracellular concentration is stable. The concentration of PAs in cancer cells is significantly increased to promote and sustain their rapid proliferation. Over the years, synthetic PAs, which differ in...

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Autores principales: Artemiy Nichugovskiy, Gian Cesare Tron, Mikhail Maslov
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Publicado: MDPI AG 2021
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spelling oai:doaj.org-article:414c51bcd7124ffd8c640ef76c522c662021-11-11T18:33:28ZRecent Advances in the Synthesis of Polyamine Derivatives and Their Applications10.3390/molecules262165791420-3049https://doaj.org/article/414c51bcd7124ffd8c640ef76c522c662021-10-01T00:00:00Zhttps://www.mdpi.com/1420-3049/26/21/6579https://doaj.org/toc/1420-3049Biogenic polyamines (PAs) are involved in the growth and development of normal cells, and their intracellular concentration is stable. The concentration of PAs in cancer cells is significantly increased to promote and sustain their rapid proliferation. Over the years, synthetic PAs, which differ in their structure, have demonstrated high antitumor activity and are involved in clinical trials. The chemical synthesis of PAs and their conjugates require the correct choice of synthetic pathways—methods for constructing conjugates and the orthogonal protection of amino groups. The most common methods of synthesis of PA conjugates are acylation of regioselectively protected PAs or their alkylation under the conditions of the Fukuyama reaction. One of the most promising methods of PA synthesis is the use of a multicomponent Ugi reaction, which allows various PAs to be obtained in high yields. In this review, we describe and analyze various approaches that are used in the synthesis of polyamines and their conjugates.Artemiy NichugovskiyGian Cesare TronMikhail MaslovMDPI AGarticlepolyaminespolyamine conjugatesantitumor activityantimalarial agentsUgi reactionOrganic chemistryQD241-441ENMolecules, Vol 26, Iss 6579, p 6579 (2021)
institution DOAJ
collection DOAJ
language EN
topic polyamines
polyamine conjugates
antitumor activity
antimalarial agents
Ugi reaction
Organic chemistry
QD241-441
spellingShingle polyamines
polyamine conjugates
antitumor activity
antimalarial agents
Ugi reaction
Organic chemistry
QD241-441
Artemiy Nichugovskiy
Gian Cesare Tron
Mikhail Maslov
Recent Advances in the Synthesis of Polyamine Derivatives and Their Applications
description Biogenic polyamines (PAs) are involved in the growth and development of normal cells, and their intracellular concentration is stable. The concentration of PAs in cancer cells is significantly increased to promote and sustain their rapid proliferation. Over the years, synthetic PAs, which differ in their structure, have demonstrated high antitumor activity and are involved in clinical trials. The chemical synthesis of PAs and their conjugates require the correct choice of synthetic pathways—methods for constructing conjugates and the orthogonal protection of amino groups. The most common methods of synthesis of PA conjugates are acylation of regioselectively protected PAs or their alkylation under the conditions of the Fukuyama reaction. One of the most promising methods of PA synthesis is the use of a multicomponent Ugi reaction, which allows various PAs to be obtained in high yields. In this review, we describe and analyze various approaches that are used in the synthesis of polyamines and their conjugates.
format article
author Artemiy Nichugovskiy
Gian Cesare Tron
Mikhail Maslov
author_facet Artemiy Nichugovskiy
Gian Cesare Tron
Mikhail Maslov
author_sort Artemiy Nichugovskiy
title Recent Advances in the Synthesis of Polyamine Derivatives and Their Applications
title_short Recent Advances in the Synthesis of Polyamine Derivatives and Their Applications
title_full Recent Advances in the Synthesis of Polyamine Derivatives and Their Applications
title_fullStr Recent Advances in the Synthesis of Polyamine Derivatives and Their Applications
title_full_unstemmed Recent Advances in the Synthesis of Polyamine Derivatives and Their Applications
title_sort recent advances in the synthesis of polyamine derivatives and their applications
publisher MDPI AG
publishDate 2021
url https://doaj.org/article/414c51bcd7124ffd8c640ef76c522c66
work_keys_str_mv AT artemiynichugovskiy recentadvancesinthesynthesisofpolyaminederivativesandtheirapplications
AT giancesaretron recentadvancesinthesynthesisofpolyaminederivativesandtheirapplications
AT mikhailmaslov recentadvancesinthesynthesisofpolyaminederivativesandtheirapplications
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