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Review

Recent Advances in the Synthesis of Polyamine Derivatives and Their Applications

by
Artemiy Nichugovskiy
1,
Gian Cesare Tron
2 and
Mikhail Maslov
1,*
1
Lomonosov Institute of Fine Chemical Technologies, MIREA—Russian Technological University, 86 Vernadsky Ave., 119571 Moscow, Russia
2
Dipartimento di Scienza del Farmaco, Università del Piemonte Orientale, Largo Donegani 2, 28100 Novara, Italy
*
Author to whom correspondence should be addressed.
Molecules 2021, 26(21), 6579; https://doi.org/10.3390/molecules26216579
Submission received: 30 September 2021 / Revised: 22 October 2021 / Accepted: 26 October 2021 / Published: 30 October 2021
(This article belongs to the Special Issue Polyamine Drug Discovery)
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Abstract

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.
Keywords: polyamines; polyamine conjugates; antitumor activity; antimalarial agents; Ugi reaction polyamines; polyamine conjugates; antitumor activity; antimalarial agents; Ugi reaction
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MDPI and ACS Style

Nichugovskiy, A.; Tron, G.C.; Maslov, M. Recent Advances in the Synthesis of Polyamine Derivatives and Their Applications. Molecules 2021, 26, 6579. https://doi.org/10.3390/molecules26216579

AMA Style

Nichugovskiy A, Tron GC, Maslov M. Recent Advances in the Synthesis of Polyamine Derivatives and Their Applications. Molecules. 2021; 26(21):6579. https://doi.org/10.3390/molecules26216579

Chicago/Turabian Style

Nichugovskiy, Artemiy, Gian Cesare Tron, and Mikhail Maslov. 2021. "Recent Advances in the Synthesis of Polyamine Derivatives and Their Applications" Molecules 26, no. 21: 6579. https://doi.org/10.3390/molecules26216579

APA Style

Nichugovskiy, A., Tron, G. C., & Maslov, M. (2021). Recent Advances in the Synthesis of Polyamine Derivatives and Their Applications. Molecules, 26(21), 6579. https://doi.org/10.3390/molecules26216579

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