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RESEARCH PRODUCT

ChemInform Abstract: Advances in Indolo[2,3-a]carbazole Chemistry: Design and Synthesis of Protein Kinase C and Topoisomerase I Inhibitors

Young‐shin KimUlf PindurFarokh Mehrabani

subject

chemistry.chemical_classificationchemistry.chemical_compoundEnzymebiologyChemistryStereochemistryCarbazoleTopoisomerasebiology.proteinMolecular bindingGeneral MedicineTopoisomerase-I InhibitorProtein kinase C

description

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.

https://doi.org/10.1002/chin.199918300