Cationic porphyrins and analogues as new DNA topoisomerase I and II inhibitors.
A series of cationic porphyrins, and analogues such as cationic corroles and phthalocyanines were found to have biological activities towards topoisomerases I and II in vitro. Cationic porphyrins and phthalocyanines do not induce Topo I-DNA covalent complexes but inhibit topoisomerase I by direct binding to DNA, which limits topoisomerase I access to the DNA substrate. The lowest concentration where an inhibition effect is clearly visible of some derivatives is between 0.1 and 0.6 microM. Furthermore, some complexes were found to inhibit the activity of the topoisomerase II.
Shuai
Li
L
College of Chemistry and Molecular Sciences, Wuhan University, Hubei, Wuhan 430072, P. R. China.
Wang
Shaoru
S
Zhang
Lixia
L
Fu
Boqiao
B
Zhou
Xiang
X
D002412:Cations / Q000737:chemistry* / Q000494:pharmacology; D053837:DNA Cleavage; D004264:DNA Topoisomerases, Type I / Q000378:metabolism; D004250:DNA Topoisomerases, Type II / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D007364:Intercalating Agents / Q000737:chemistry / Q000494:pharmacology; D011166:Porphyrins / Q000737:chemistry* / Q000494:pharmacology; D011485:Protein Binding; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors
D002412:Cations; D004791:Enzyme Inhibitors; D007364:Intercalating Agents; D011166:Porphyrins; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors; D004264:DNA Topoisomerases, Type I; D004250:DNA Topoisomerases, Type II