3-Aryl-N-aminoylsulfonylphenyl-1H-pyrazole-5-carboxamides: a new class of selective Rac inhibitors

被引：23

作者：

Ferri, Nicola ^{[1
]}

Bernini, Sergio Kevin ^{[1
]}

Corsini, Alberto ^{[1
]}

Clerici, Francesca ^{[2
]}

Erba, Emanuela ^{[2
]}

Stragliotto, Stefano ^{[2
]}

Contini, Alessandro ^{[2
]}

机构：

[1] Univ Milan, Dipartimento Sci Farmacol & Biomol, I-20133 Milan, Italy

[2] Univ Milan, Dipartimento Sci Farmaceut, Sez Chim Gen & Organ A Marchesini, I-20133 Milan, Italy

来源：

MEDCHEMCOMM | 2013年 / 4卷 / 03期

关键词：

SMALL-MOLECULE INHIBITOR; VASCULAR-PERMEABILITY; GTPASE; ACTIVATION; INTEGRINS; ADHESION; PATHWAY; RHO;

D O I：

10.1039/c2md20328f

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Through a computational approach, five new compounds with potent and selective Rac inhibitory activity were identified. In particular, compound 4 was shown to selectively inhibit Rac activity in a concentration-dependent manner by affecting the GEF-dependent GDP-GTP exchange. This compound was more potent than the original inhibitors previously identified.

引用

页码：537 / 541

页数：5

共 50 条

[41] Synthesis and anti-TMV activity of novel N-(3-alkyl-1H-pyrazol-4-yl)-3-alkyl-4-substituted-1H-pyrazole-5-carboxamides
Zhang, Da Qiang
Xu, Gao Fei
Fan, Zhi Jin
Wang, Dao Quan
Yang, Xin Ling
Yuan, De Kai
CHINESE CHEMICAL LETTERS, 2012, 23 (06) : 669 - 672
[42] Synthesis and anti-TMV activity of novel N-(3-alkyl-1H-pyrazol-4-yl)-3-alkyl-4-substituted-1H-pyrazole-5-carboxamides
Da Qiang Zhang~a
ChineseChemicalLetters, 2012, 23 (06) : 669 - 672
[43] Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists
Seong, Churl Min
Park, Woo Kyu
Park, Chul Min
Kong, Jae Yang
Park, No Sang
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2008, 18 (02) : 738 - 743
[44] Synthesis and bioactivity evaluation of ethyl 1-arylmethyl-3-aryl-1-H-pyrazole-5-carboxylate derivatives
Ding, Xiao-Ling
Meng, Ning
Xia, Yong
Wang, Li-Juan
Zhang, Xiao-Feng
Zhao, Bao-Xiang
Miao, Jun-Ying
CHINESE JOURNAL OF ORGANIC CHEMISTRY, 2007, 27 (12) : 1542 - 1546
[45] 5,5′-Dimethyl-N,N′-(iminodiethylene)-bis(1H-pyrazole-3-carboxamide)
Hu, Jing
Chen, Guofeng
Ma, Guochun
Song, Hongguang
ACTA CRYSTALLOGRAPHICA SECTION E-STRUCTURE REPORTS ONLINE, 2007, 63 : O4806 - U5969
[46] Optimization of Novel 1-Methyl-1H-Pyrazole-5-carboxamides Leads to High Potency Larval Development Inhibitors of the Barber's Pole Worm
Le, Thuy G.
Kundu, Abhijit
Ghoshal, Atanu
Nguyen, Nghi H.
Preston, Sarah
Jiao, Yaqing
Ruan, Banfeng
Xue, Lian
Huang, Fei
Keiser, Jennifer
Hofmann, Andreas
Chang, Bill C. H.
Garcia-Bustos, Jose
Jabbar, Abdul
Wells, Timothy N. C.
Palmer, Michael J.
Gasser, Robin B.
Baell, Jonathan B.
JOURNAL OF MEDICINAL CHEMISTRY, 2018, 61 (23) : 10875 - 10894
[47] N-(3-(Phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck:: Structure, synthesis and SAR
Deak, Holly L.
Newcomb, John R.
Nunes, Joseph J.
Boucher, Christina
Cheng, Alan C.
DiMauro, Erin F.
Epstein, Linda F.
Gallant, Paul
Hodous, Brian L.
Huang, Xin
Lee, Josie H.
Patel, Vinod F.
Schneider, Stephen
Turci, Susan M.
Zhu, Xiaotian
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2008, 18 (03) : 1172 - 1176
[48] Synthesis of some novel 1-aryl-1H-1,2,3-triazole-4-carboxamides and ethyl 1-aryl-5-(1,2,3-triazol-1-yl)-1H-pyrazole-4-carboxylates
Avigliano, Marialuce
De Francesco, Debora
Brizzi, Antonella
Paolino, Marco
Corelli, Federico
Mugnaini, Claudia
ARKIVOC, 2023, : 1 - 11
[49] A NEW SYNTHESIS OF 1-ARYL-5-CYANO-1H-PYRAZOLE-4-CARBOXYLIC ACID, ETHYL-ESTERS
BECK, JR
ACKMANN, SA
STASZAK, MA
WRIGHT, FL
JOURNAL OF HETEROCYCLIC CHEMISTRY, 1988, 25 (03) : 955 - 958
[50] Crystal structure of N '-diphenylmethylidene-5-methyl-1H-pyrazole-3-carbohydrazide
Karrouchi, Khalid
Ansar, M'hammed
Radi, Smaail
Saadi, Mohamed
El Ammari, Lahcen
ACTA CRYSTALLOGRAPHICA SECTION E-CRYSTALLOGRAPHIC COMMUNICATIONS, 2015, 71 : O890 - U632

← 1 2 3 4 5 →