Аннотация:
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.
Образец цитирования:
N. A. Lozinskaya, N. A. Maximova, D. R. Bazanov, S. E. Sosonyuk, B. Wobith, N. A. Zefirov, E. V. Kharitonashvili, O. N. Zefirova, S. A. Kuznetsov, M. V. Proskurnina, “Synthesis and biotesting of new carrier prodrugs of 2-methoxyestradiol”, Mendeleev Commun., 30:1 (2020), 7–9