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.
Highlights
[6,7].Of note, the lack of PAs in cells leads to the activation of apoptosis; a promising anticancer target is the inhibition of PA synthesis [8,9]
We describe and analyze various approaches that have been used in the synthesis review, we describe and analyze various approaches that have been used in the synthesis of polyamines polyamines and and their their conjugates
The stereoselective synthesis of PA precursors from non-activated esters and α,ω-diamines catalyzed by Candida antarctica lipase (CAL) in organic solvent gave bis-(amidoesters) as the only product [30]
Summary
An excess of PAs leads to programmed cell death—apoptosis [6,7].Of note, the lack of PAs in cells leads to the activation of apoptosis; a promising anticancer target is the inhibition of PA synthesis [8,9]. The lack of PAs in cells leads to the activation of apoptosis; a promising anticancer target is the inhibition of PA synthesis [8,9]. PTS still remains, but the is known to involve the absorption and withdrawal of PAs, which are necessary for their most preferred transportstructure is linked to endocytosis, pinocytosis, and processing. PTS can be considered a target for cytotoxic polyamine-conjugated polyamine-conjugateddrugs drugs[15] In this regard, PAs are potential influencers on cellular processes. We describe and analyze various approaches that have been used in the synthesis review, we describe and analyze various approaches that have been used in the synthesis of polyamines polyamines and and their their conjugates
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