7661-12-3Relevant articles and documents
Arylamide as Potential Selective Inhibitor for Matrix Metalloproteinase 9 (MMP9): Design, Synthesis, Biological Evaluation, and Molecular Modeling
Al-Najjar, Belal,Dewa, Sangga P.,Hariono, Maywan,Jati, Benedictus W.,Jenie, Riris I.,Julianus, Jeffry,Nugroho, Ervan S.,Nuwarda, Rina F.,Putra, Kevin C.,Qodria, Lailatul,Ramadani, Ratna D.,Rollando, Rollando,Tiara, Reynaldo,Wahab, Habibah A.,Wisnumurti, Yohanes K.,Yusuf, Muhammad
, (2020/01/21)
Previous studies have reported that compounds bearing an arylamide linked to a heterocyclic planar ring have successfully inhibited the hemopexin-like domain (PEX9) of matrix metalloproteinase 9 (MMP9). PEX9 has been suggested to be more selectively targe
Formation of acridones by ethylene extrusion in the reaction of arynes with β-lactams and dihydroquinolinones
Fang, Yuesi,Rogness, Donald C.,Larock, Richard C.,Shi, Feng
experimental part, p. 6262 - 6270 (2012/09/22)
N-Unsubstituted β-lactams react with a molecule of aryne by insertion into the amide bond to form a 2,3-dihydroquinolin-4-one, which subsequently reacts with another molecule of aryne to form an acridone by extrusion of a molecule of ethylene. 2,3-Dihydroquinolin-4-ones react under the same reaction conditions to afford identical results. This is the first example of ethylene extrusion in aryne chemistry.
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.