Zakharenko, Alexandra L’s team published research in Molecules in 2020 | 128-09-6

Molecules published new progress about Antitumor agents. 128-09-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C4H4ClNO2, Name: 1-Chloropyrrolidine-2,5-dione.

Zakharenko, Alexandra L.; Drenichev, Mikhail S.; Dyrkheeva, Nadezhda S.; Ivanov, Georgy A.; Oslovsky, Vladimir E.; Ilina, Ekaterina S.; Chernyshova, Irina A.; Lavrik, Olga I.; Mikhailov, Sergey N. published the artcile< Inhibition of tyrosyl-DNA phosphodiesterase 1 by lipophilic pyrimidine nucleosides>, Name: 1-Chloropyrrolidine-2,5-dione, the main research area is deoxyribonucleic acid repair nucleoside topoisomerase inhibitor; DNA repair; Tdp1 inhibition; nucleosides; topotecan; tyrosyl-DNA phosphodiesterase.

Inhibition of DNA repair enzymes tyrosyl-DNA phosphodiesterase 1 and poly(ADP-ribose) polymerases 1 and 2 in the presence of pyrimidine nucleoside derivatives was studied here. New effective Tdp1 inhibitors were found in a series of nucleoside derivatives possessing 2′, 3′, 5′ -tri-O-benzoyl-d-ribofuranose and 5-substituted uracil moieties and have half-maximal inhibitory concentrations (IC50) in the lower micromolar and submicromolar range. 2′, 3′, 5′-Tri-O-benzoyl-5-iodouridine manifested the strongest inhibitory effect on Tdp1 (IC50 = 0.6μM). A decrease in the number of benzoic acid residues led to a marked decline in the inhibitory activity, and pyrimidine nucleosides lacking lipophilic groups (uridine, 5-fluorouridine, 5-chlorouridine, 5-bromouridine, 5-iodouridine, and ribothymidine) did not cause noticeable inhibition of Tdp1 (IC50 > 50μM). No PARP1/2 inhibitors were found among the studied compounds (residual activity in the presence of 1 mM substances was 50-100%). Several O-benzoylated uridine and cytidine derivatives strengthened the action of topotecan on HeLa cervical cancer cells.

Molecules published new progress about Antitumor agents. 128-09-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C4H4ClNO2, Name: 1-Chloropyrrolidine-2,5-dione.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics