51458-66-3Relevant academic research and scientific papers
Guanidinium-based derivatives: Searching for new kinase inhibitors
Diez-Cecilia, Elena,Kelly, Brendan,Perez, Concepcion,Zisterer, Daniela M.,Nevin, Daniel K.,Lloyd, David G.,Rozas, Isabel
, p. 427 - 441 (2014/06/09)
Considering the structural similarities between the kinase inhibitor sorafenib and 4,4′-bis-guanidinium derivatives previously prepared by Rozas and co., which display interesting cytotoxicity in cancer cells, we have studied whether this activity could result from kinase inhibition. Five new families have been prepared consisting of unsubstituted and aryl-substituted 3,4′-bis-guanidiniums, 3,4′-bis-2-aminoimidazolinium and 3-acetamide-4′-(4-chloro-3-trifluoromethylphenyl)guanidinium derivatives. Cytotoxicity (measuring the IC50 values) and apoptosis studies in human HL-60 promyelocytic leukemia cells were carried out for these compounds. Additionally, their potential inhibitory effect was explored on a panel of kinases known to be involved in apoptotic pathways. The previously prepared cytotoxic 4,4′-bis-guanidiniums did not inhibit any of these kinases; however, some of the novel 3,4′-substituted derivatives showed a high percentage inhibition of RAF-1/MEK-1, for which the potential mode of binding was evaluated by docking studies. The interesting antitumour properties showed by these compounds open up new exciting lines of investigation for kinase inhibitors as anticancer agents and also highlights the relevance of the guanidinium moiety for protein kinase inhibitors chemical design.
Process for preparation of 3,3'- or 3,4'-diamino benzophenone
-
, (2008/06/13)
3,3'- or 3,4'-diamino benzophenone is prepared by catalytically reducing and dehalogenating, in the presence of a reduction catalyst and a dehydrohalogenation agent, a benzophenone compound or benzophenone compounds of the general formula STR1 in which X is a halogen atom at position 2 or 4 of the benzene ring and Y is hydrogen or a halogen atom and in which the nitro group is at position 3' or 4' of the benzene ring if Y is hydrogen, while Y is at position 4' and the nitro group is at position 3' of the benzene ring if Y is a halogen atom.
