Optimization of 4-Phenylamino-3-quinolinecarbonitriles as Potent Inhibitors of Src Kinase Activity was written by Boschelli, Diane H.;Ye, Fei;Wang, Yanong D.;Dutia, Minu;Johnson, Steve L.;Wu, Biqi;Miller, Karen;Powell, Dennis W.;Yaczko, Deanna;Young, Mairead;Tischler, Mark;Arndt, Kim;Discafani, Carolyn;Etienne, Carlo;Gibbons, Jay;Grod, Janet;Lucas, Judy;Weber, Jennifer M.;Boschelli, Frank. And the article was included in Journal of Medicinal Chemistry in 2001.Computed Properties of C7H16N2 This article mentions the following:
Subsequent to the discovery of 4-[(2,4-dichlorophenyl)amino]-6,7-dimethoxy-3-quinolinecarbonitrile as an inhibitor of Src kinase activity (IC50 = 30 nM), several addnl. analogs were prepared Optimization of the C-4 anilino group led to I [R = Me]. Replacement of the methoxy group at C-7 with a 3-(morpholin-4-yl)propoxy group provided I [R = morpholinopropyl], resulting in increased inhibition of both Src kinase activity and Src-mediated cell proliferation. Analogs of I [R = morpholinopropyl] with other trisubstituted anilines at C-4 were also potent Src inhibitors, and the propoxy group was preferred over ethoxy, butoxy, or pentoxy. Replacement of the morpholine group with a 4-methylpiperazine group provided I [R = 4-methylpiperazinopropyl], which had an IC50 of 1.2 nM in the Src enzymic assay, an IC50 of 100 nM for the inhibition of Src-dependent cell proliferation and was selective for Src over non-Src family kinases. I [R = 4-methylpiperazinopropyl], which had higher 1 and 4 h plasma levels than I [R = 4-morpholinopropyl], effectively inhibited tumor growth in xenograft models. In the experiment, the researchers used many compounds, for example, 1-Propylpiperazine (cas: 21867-64-1Computed Properties of C7H16N2).
1-Propylpiperazine (cas: 21867-64-1) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Computed Properties of C7H16N2
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics