title: Advances in indolo[2,3-a]carbazole chemistry: design and synthesis of protein kinase C and topoisomerase I inhibitors.
abstract: Indolo[2,3-a]carbazoles, their pyrrolo[3,4-c]anellated variants and structurally closely related bisindolylmaleimides represent a biologically highly interesting class of natural compounds which are potential anticancer agents. According to the ongoing literature new and efficient synthetic methods yield a great variety of these compounds which have been reported in detail. The biological activities and the inhibitory activities against the target enzymes protein kinase C and topoisomerase I are also discussed including structure activity relationships. A molecular binding model of the protein kinase C inhibitors with the target enzyme at the atomic level is presented and supported by X-ray crystallographic structures and by molecular modelling studies.
authors.affiliation: Institute of Pharmacy, Faculty of Chemistry and Pharmacy University of Mainz, Mainz D-55099 Germany.
authors.forename: U
authors.initials: U
authors.lastname: Pindur
authors.forename: Y S
authors.initials: YS
authors.lastname: Kim
authors.forename: F
authors.initials: F
authors.lastname: Mehrabani
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002227:Carbazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D008301:Maleimides / Q000138:chemical synthesis / Q000494:pharmacology; D011493:Protein Kinase C / Q000037:antagonists & inhibitors*; D011758:Pyrroles / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship; D059004:Topoisomerase I Inhibitors
chemical_list: D000970:Antineoplastic Agents; D002227:Carbazoles; D007211:Indoles; D008301:Maleimides; D011758:Pyrroles; D059004:Topoisomerase I Inhibitors; D011493:Protein Kinase C