Detalles de la búsqueda
1.
Discovery of 4-(4-aminopyrazolo[1,5-a][1,3,5]triazin-8-yl)benzamides as novel, highly potent and selective, orally bioavailable inhibitors of Tyrosine Threonine Kinase, TTK.
Bioorg Med Chem Lett
; 26(15): 3562-6, 2016 08 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-27335255
2.
Design and optimization of (3-aryl-1H-indazol-6-yl)spiro[cyclopropane-1,3'-indolin]-2'-ones as potent PLK4 inhibitors with oral antitumor efficacy.
Bioorg Med Chem Lett
; 26(19): 4625-4630, 2016 10 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-27592744
3.
Discovery of inhibitors of the mitotic kinase TTK based on N-(3-(3-sulfamoylphenyl)-1H-indazol-5-yl)-acetamides and carboxamides.
Bioorg Med Chem
; 22(17): 4968-97, 2014 Sep 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-25043312
4.
Mode of action, in vitro activity, and in vivo efficacy of AFN-1252, a selective antistaphylococcal FabI inhibitor.
Antimicrob Agents Chemother
; 56(11): 5865-74, 2012 Nov.
Artículo
en Inglés
| MEDLINE | ID: mdl-22948878
5.
Dimerization of ß-tryptase inhibitors, does it work for both basic and neutral P1 groups?
Bioorg Med Chem Lett
; 22(9): 3370-6, 2012 May 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-22483389
6.
Structure-based library design and the discovery of a potent and selective mast cell ß-tryptase inhibitor as an oral therapeutic agent.
Bioorg Med Chem Lett
; 22(2): 1049-54, 2012 Jan 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-22192588
7.
Spiro-naphthyridinone piperidines as inhibitors of S. aureus and E. coli enoyl-ACP reductase (FabI).
Bioorg Med Chem Lett
; 19(18): 5355-8, 2009 Sep 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-19682901
8.
2,3,4,5-Tetrahydro-1H-pyrido[2,3-b and e][1,4]diazepines as inhibitors of the bacterial enoyl ACP reductase, FabI.
Bioorg Med Chem Lett
; 19(18): 5359-62, 2009 Sep 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-19682900
9.
Discovery of Pyrazolo[1,5-a]pyrimidine TTK Inhibitors: CFI-402257 is a Potent, Selective, Bioavailable Anticancer Agent.
ACS Med Chem Lett
; 7(7): 671-5, 2016 Jul 14.
Artículo
en Inglés
| MEDLINE | ID: mdl-27437075
10.
The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents.
J Med Chem
; 58(1): 130-46, 2015 Jan 08.
Artículo
en Inglés
| MEDLINE | ID: mdl-24867403
11.
The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor agent.
J Med Chem
; 58(1): 147-69, 2015 Jan 08.
Artículo
en Inglés
| MEDLINE | ID: mdl-25723005
12.
The Discovery of Orally Bioavailable Tyrosine Threonine Kinase (TTK) Inhibitors: 3-(4-(heterocyclyl)phenyl)-1H-indazole-5-carboxamides as Anticancer Agents.
J Med Chem
; 58(8): 3366-92, 2015 Apr 23.
Artículo
en Inglés
| MEDLINE | ID: mdl-25763473
13.
Molecular structures of human factor Xa complexed with ketopiperazine inhibitors: preference for a neutral group in the S1 pocket.
J Med Chem
; 46(5): 685-90, 2003 Feb 27.
Artículo
en Inglés
| MEDLINE | ID: mdl-12593649
14.
Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand.
J Med Chem
; 46(5): 681-4, 2003 Feb 27.
Artículo
en Inglés
| MEDLINE | ID: mdl-12593648
15.
In vitro activity (MICs and rate of kill) of AFN-1252, a novel FabI inhibitor, in the presence of serum and in combination with other antibiotics.
J Chemother
; 25(1): 18-25, 2013 Feb.
Artículo
en Inglés
| MEDLINE | ID: mdl-23433440
16.
The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents.
J Med Chem
; 56(15): 6069-87, 2013 Aug 08.
Artículo
en Inglés
| MEDLINE | ID: mdl-23829549
17.
Design, synthesis, and biological activity of potent and selective inhibitors of mast cell tryptase.
Bioorg Med Chem Lett
; 15(11): 2734-7, 2005 Jun 02.
Artículo
en Inglés
| MEDLINE | ID: mdl-15911249
18.
Structure based design of 4-(3-aminomethylphenyl)piperidinyl-1-amides: novel, potent, selective, and orally bioavailable inhibitors of betaII tryptase.
Bioorg Med Chem
; 13(8): 2859-72, 2005 Apr 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-15781396
19.
Novel pyrazinone inhibitors of mast cell tryptase: synthesis and SAR evaluation.
Bioorg Med Chem Lett
; 14(19): 4819-23, 2004 Oct 04.
Artículo
en Inglés
| MEDLINE | ID: mdl-15341931
20.
Optimization of the beta-aminoester class of factor Xa inhibitors. Part 1: P(4) and side-chain modifications for improved in vitro potency.
Bioorg Med Chem Lett
; 12(12): 1667-70, 2002 Jun 17.
Artículo
en Inglés
| MEDLINE | ID: mdl-12039586