1094276-76-2Relevant academic research and scientific papers
Search for inhibitors of bacterial and human protein kinases among derivatives of diazepines[1,4] annelated with maleimide and indole cycles
Danilenko, Valery N.,Simonov, Alexander Y.,Lakatosh, Sergey A.,Kubbutat, Michael H. G.,Totzke, Frank,Sch?chtele, Christoph,Elizarov, Sergey M.,Bekker, Olga B.,Printsevskaya, Svetlana S.,Luzikov, Yuryi N.,Reznikova, Marina I.,Shtil, Alexander A.,Preobrazhenskaya, Maria N.
, p. 7731 - 7736 (2008)
Aminomethylation of 9b,10-dihydro-1H-indolo[1,7:4,5,6]pyrrolo[3,4:2,3][1,4] diazepino-[1,7-a]indole-1,3(2H)-diones or 1H-indolo[1,7:4,5,6]pyrrolo[3,4:2,3] [1,4]diazepino[1,7-a]indole-1,3(2H)-diones resulted in dialkylaminomethyl derivatives. Alkylation of the nitrogen atom of maleimide moiety of polyannelated diazepines with 1,3-dibromopropane and subsequent reaction with thiourea or its N-alkyl derivatives gave isothiourea-carrying compounds. The compounds containing isothiourea moiety were active against individual human serine/threonine and tyrosine kinases at low micromolar concentrations. Dialkylaminomethyl derivatives of diazepines sensitized Streptomyces lividans with overexpressed aminoglycoside phosphotransferase type VIII (aphVIII) to kanamycin by inhibiting serine/threonine kinase(s) mediated aphVIII phosphorylation.
