This review comprehensively describes the recent advances in the synthesis and pharmacological evaluation of steroid polyamines squalamine, trodusquemine, ceragenins, claramine, and their diverse analogs and derivatives, with a special focus on their complete synthesis from cholic acids, as well as an antibacterial and antiviral, neuroprotective, antiangiogenic, antitumor, antiobesity and weight-loss activity, antiatherogenic, regenerative, and anxiolytic properties. Trodusquemine is the most-studied small-molecule allosteric PTP1B inhibitor. The discovery of squalamine as the first representative of a previously unknown class of natural antibiotics of animal origin stimulated extensive research of terpenoids (especially triterpenoids) comprising polyamine fragments. During the last decade, this new class of biologically active semisynthetic natural product derivatives demonstrated the possibility to form supramolecular networks, which opens up many possibilities for the use of such structures for drug delivery systems in serum or other body fluids.

Department of Chemistry of Natural Compounds University of Chemistry and Technology Prague Technicka' 5 Prague 6 16628 Prague Czech Republic

Laboratory of Metabotropic Drugs Scientific Center for Innovative Drugs Volgograd State Medical University Novorossiyskaya St 39 400087 Volgograd Russia

Ufa Institute of Chemistry UFA Federal Research Centre of the Russian Academy of Sciences Pr Oktyabrya 450054 Ufa Russia

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