13910-55-9Relevant academic research and scientific papers
Insight into structural requirements for selective and/or dual CXCR3 and CXCR4 allosteric modulators
Kolari?, Anja,?vajger, Urban,Toma?i?, Tihomir,Brox, Regine,Frank, Theresa,Minovski, Nikola,Tschammer, Nuska,Anderluh, Marko
, p. 68 - 90 (2018/05/26)
Based on the previously published pyrazolopyridine-based hit compound for which negative allosteric modulation of both CXCR3 and CXCR4 receptors was disclosed, we designed, synthesized and biologically evaluated a set of novel, not only negative, but also positive allosteric modulators with preserved pyrazolopyridine core. Compound 9e is a dual negative modulator, inhibiting G protein activity of both receptors. For CXCR4 receptor para-substituted aromatic group of compounds distinguishes between negative and positive modulation. Para-methoxy substitution leads to functional antagonism, while para-chloro triggers agonism. Additionally, we discovered that chemotaxis is not completely correlated with G protein pathways. This is the first work in which we have on a series of compounds successfully demonstrated that it is possible to produce selective as well as dual-acting modulators of chemokine receptors, which is very promising for future research in the field of discovery of selective or dual modulators of chemokine receptors.
Design, synthesis and prostate cancer cell-based studies of analogs of the Rho/MKL1 transcriptional pathway inhibitor, CCG-1423
Evelyn, Chris R.,Bell, Jessica L.,Ryu, Jenny G.,Wade, Susan M.,Kocab, Andrew,Harzdorf, Nicole L.,Hollis Showalter,Neubig, Richard R.,Larsen, Scott D.
scheme or table, p. 665 - 672 (2010/06/21)
We recently identified bis(amide) CCG-1423 (1) as a novel inhibitor of RhoA/C-mediated gene transcription that is capable of inhibiting invasion of PC-3 prostate cancer cells in a Matrigel model of metastasis. An initial structure-activity relationship study focusing on bioisosteric replacement of the amides and conformational restriction identified two compounds, 4g and 8, with improved selectivity for inhibition of RhoA/C-mediated gene transcription and attenuated cytotoxicity relative to 1. Both compounds were also capable of inhibiting cell invasion with equal efficacy to 1 but with less attendant cytotoxicity.
Selective monoformylation of 1,3-diaminopropane derivatives
Orelli, Liliana R.,Garcia, Maria B.,Niemevz, Fernando,Perillo, Isabel A.
, p. 1819 - 1833 (2007/10/03)
A general procedure for regiospecific construction of N-aryl-N'-formyl- 1,3-diaminopropanes 2 (R=H) by selective monoformylation of N-(3- aminopropyl)arylamines 1 is described. Compounds 1 are readily obtained with high yields by aminolysis of 3-bromoprop
