Synthesis and Biological Activity of Novel Comenic Acid Derivatives Containing Isoxazole and Isothiazole Moieties

Methyl 5-hydroxy-4-oxo-4H-pyran-2-carboxylate was synthesized by esterification of methanol with comenic acid under acidic catalysis. The obtained ester was alkylated with 3-(chloromethyl)-5-phenylisoxazole and 4,5-dichloro-3-(chloromethyl)isothiazole to afford corresponding conjugates containing is...

Full description

Saved in:
Bibliographic Details
Published in:Natural product communications 2018-11, Vol.13 (11)
Main Authors: Kletskov, Alexey V., Potkin, Vladimir I., Kolesnik, Irina A., Petkevich, Sergey K., Kvachonak, Anastasia V., Dosina, Margarita O., Loiko, Diana O., Larchenko, Maria V., Pashkevich, Svetlana G., Kulchitsky, Vladimir A.
Format: Article
Language:English
Citations: Items that this one cites
Items that cite this one
Online Access:Request full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Methyl 5-hydroxy-4-oxo-4H-pyran-2-carboxylate was synthesized by esterification of methanol with comenic acid under acidic catalysis. The obtained ester was alkylated with 3-(chloromethyl)-5-phenylisoxazole and 4,5-dichloro-3-(chloromethyl)isothiazole to afford corresponding conjugates containing isoxazole and isothiazole moieties which then were transformed into water-soluble Li-salts. During the bioassays of synthesized isoxazole and isothiazole derivatives of comenic acid in mixtures with first-line antitumor drug Temobel (Temozolomid) used in brain tumors chemotherapy, a synergetic effect was observed.
ISSN:1934-578X
1555-9475
DOI:10.1177/1934578X1801301124