Title:Semi-Synthetic Derivatives of Heliomycin with an Antiproliferative Potency
VOLUME: 13 ISSUE: 4
Author(s):Georgy Y. Nadysev, Alexander S. Tikhomirov, Lyubov G. Dezhenkova and Andrey E. Shchekotikhin*
Affiliation:Gause Institute of New Antibiotics, 11 B. Pirogovskaya Street, Moscow 119021, Gause Institute of New Antibiotics, 11 B. Pirogovskaya Street, Moscow 119021, Gause Institute of New Antibiotics, 11 B. Pirogovskaya Street, Moscow 119021, Gause Institute of New Antibiotics, 11 B. Pirogovskaya Street, Moscow 119021
Keywords:Aminomethylation, anticancer agents, heliomycin, improved solubility, Mannich reaction, resistomycin.
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.
