Semi-Synthetic Derivatives of Heliomycin with an Antiproliferative Potency

Abstract

Background: Heliomycin (resistomycin), an antibiotic with broad spectra of biological activities including antimicrobial, antifungal, antiviral, and antiproliferative. However, an extremely low solubility in aqueous media and in the majority of organic solvents limits its practical application.

Objective: Due to a high practical potential of heliomycin, new routes of structural modification are strongly required to improve its solubility.

Conclusion: The patent claims a series of 4-aminomethyl derivatives of heliomycin as well as a pharmaceutical composition based on it. Application of Mannich aminomethylation allowed to diversify the structure of initial antibiotic and to obtain the derivatives with significantly improved water solubility and a potent antiproliferative efficacy.

Keywords: Aminomethylation; Mannich reaction; anticancer agents; heliomycin; improved solubility; resistomycin..