Literature summary for 5.6.2.1 extracted from

Chaudhuri, P.; Majumder, H.K.; Bhattacharya, S.
Synthesis, DNA binding, and Leishmania topoisomerase inhibition activities of a novel series of anthra[1,2-d]imidazole-6,11-dione derivatives (2007), J. Med. Chem., 50, 2536-2540.

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Application

Application	Comment	Organism
drug development	to identify new molecular targets for antiparasitic drugs, attention focuses on DNA topoisomerases	Leishmania donovani

Inhibitors

Inhibitors	Comment	Organism	Structure
2-pyridyl-1H-anthra[1,2-d]imidazole-6,11-dione	The hypochromicity observed on DNA addition is too low for determination of binding constants	Leishmania donovani
3-pyridyl-1H-anthra[1,2-d]imidazole-6,11-dione	The hypochromicity observed on DNA addition is too low for determination of binding constants	Leishmania donovani
4-[(3-(1-imidazolyl))propyloxy]phenyl-1H-anthra[1,2-d]imidazole-6,11-dione	shows strong DNA binding	Leishmania donovani
4-[(3-(1-tetrazolyl))propoxy]phenyl-1H-anthra[1,2-d]imidazole-6,11-dione	shows weak DNA binding	Leishmania donovani
4-[(3-(4-(2-hydroxyethyl)-1-piperazinyl))propyloxy]phenyl-1H-anthra[1,2-d]imidazole-6,11-dione	shows strong DNA binding	Leishmania donovani
4-[(3-(4-methyl-1-piperazinyl))propyloxy]phenyl-1H-anthra-[1,2-d]imidazole-6,11-dione	shows strong DNA binding	Leishmania donovani
4-[(3-(4-morpholinyl))propyloxy]phenyl-1H-anthra[1,2-d]imidazole-6,11-dione	shows weak DNA binding	Leishmania donovani
4-[(3-diethylamino)propyloxy]phenyl-1H-anthra[1,2-d]imidazole-6,11-dione	shows strong DNA binding	Leishmania donovani
4-[(3-dimethylamino)propyloxy]phenyl-1H-anthra[1,2-d]imidazole-6,11-dione	shows strong DNA binding	Leishmania donovani
camptothecin	well-known topo I poison	Leishmania donovani
additional information	Novel series of anthra[1,2-d]imidazole-6,11-dione derivatives, benzimidazole and anthraquinone derivatives are known topoisomerase inhibitors, synthesized nine imidazole-fused anthraquinone derivatives. The inhibition activity of the drugs is compared to that of the standard topo I poison cpt. Compounds with tetrazole, imidazole, or morpholine side chains exhibit potent inhibition activity against the parasitic enzyme, with activity significantly higher than that shown by camptothecin	Leishmania donovani

Organism

Organism	UniProt	Comment	Textmining
Leishmania donovani	-	unicellular kinetoplastid protozoan parasite	-

Synonyms

Synonyms	Comment	Organism
Topo I	-	Leishmania donovani
Topoisomerase I	-	Leishmania donovani

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Release 2023.1 (January 2023)