以二硝基芥子气为N端片段的新型碳环类左旋托品。拓扑异构酶的抑制作用。

New carbocyclic lexitropsins with dinitromustard as N-terminal fragment. Inhibition of topoisomerases.

作者信息

Markowska Agnieszka, Bielawska Anna, Bielawski Krzysztof, Midura-Nowaczek Krystyna

机构信息

Department of Organic Chemistry, Drug Technology Medical Academy of Bialystok, 2c Mickiewicza Str., 15-230 Białystok, Poland.

出版信息

Acta Pol Pharm. 2003 Mar-Apr;60(2):119-21.

PMID:13678319

Abstract

A series of carbocyclic lexitropsins was evaluated for their capacity to inhibit human topoisomerases I and II. The synthesized compounds were carbocyclic oligopeptides with dinitromustard as N-terminal fragment. In the topoisomerases I and II assays, the relaxation of DNA were inhibited with all four compounds. This inhibition was directly proportional to the compound concentration.

摘要

对一系列碳环类左托普辛进行了评估，以确定它们抑制人类拓扑异构酶I和II的能力。合成的化合物是带有二硝基芥子气作为N端片段的碳环寡肽。在拓扑异构酶I和II检测中，所有四种化合物均抑制了DNA的松弛。这种抑制作用与化合物浓度成正比。