Synthesis and biotesting of new carrier prodrugs of 2-methoxyestradiol

Autor:	Sergey A. Kuznetsov, Natalia A. Maximova, N. A. Zefirov, N. A. Lozinskaya, Birgit Wobith, Marina V. Proskurnina, Elena V. Kharitonashvili, Daniil R. Bazanov, Olga N. Zefirova, S. E. Sosonyuk
Rok vydání:	2020
Předmět:	A549 cell GTP' Molecular model 010405 organic chemistry Chemistry In vitro toxicology General Chemistry Prodrug 010402 general chemistry 01 natural sciences 0104 chemical sciences Biochemistry Cancer cell medicine 2-Methoxyestradiol Cytotoxicity medicine.drug
Zdroj:	Mendeleev Communications. 30:7-9
ISSN:	0959-9436
Popis:	To overcome the metabolic instability of anticancer agent 2-methoxyestradiol, two its dichloroacetylated prodrugs and three new control compounds have been synthesized and evaluated in different in vitro assays with cancer cells A549 and MCF-7. Both prodrugs demonstrated an intrinsic cytotoxicity to A549 cells with no effect on the cellular microtubule network. Molecular modeling has revealed putative weak halogen bond formation of 17-O-dichloroacetylated 2-methoxyestradiol with GTP in the a-tubulin subunit.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::d0a7fff5199ed80def2e459ef6fc9dd8 https://doi.org/10.1016/j.mencom.2020.01.002 Zobrazit plný text záznamu Full Text from ScienceDirect