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Items: 21

1.

Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor.

Perera TPS, Jovcheva E, Mevellec L, Vialard J, De Lange D, Verhulst T, Paulussen C, Van De Ven K, King P, Freyne E, Rees DC, Squires M, Saxty G, Page M, Murray CW, Gilissen R, Ward G, Thompson NT, Newell DR, Cheng N, Xie L, Yang J, Platero SJ, Karkera JD, Moy C, Angibaud P, Laquerre S, Lorenzi MV.

Mol Cancer Ther. 2017 Jun;16(6):1010-1020. doi: 10.1158/1535-7163.MCT-16-0589. Epub 2017 Mar 24.

2.

Structure-Based Design of Type II Inhibitors Applied to Maternal Embryonic Leucine Zipper Kinase.

Johnson CN, Adelinet C, Berdini V, Beke L, Bonnet P, Brehmer D, Calo F, Coyle JE, Day PJ, Frederickson M, Freyne EJ, Gilissen RA, Hamlett CC, Howard S, Meerpoel L, Mevellec L, McMenamin R, Pasquier E, Patel S, Rees DC, Linders JT.

ACS Med Chem Lett. 2014 May 23;6(1):31-6. doi: 10.1021/ml5001273. eCollection 2015 Jan 8.

3.

Fragment-based discovery of type I inhibitors of maternal embryonic leucine zipper kinase.

Johnson CN, Berdini V, Beke L, Bonnet P, Brehmer D, Coyle JE, Day PJ, Frederickson M, Freyne EJ, Gilissen RA, Hamlett CC, Howard S, Meerpoel L, McMenamin R, Patel S, Rees DC, Sharff A, Sommen F, Wu T, Linders JT.

ACS Med Chem Lett. 2014 May 23;6(1):25-30. doi: 10.1021/ml5001245. eCollection 2015 Jan 8.

4.

Potent, selective inhibitors of fibroblast growth factor receptor define fibroblast growth factor dependence in preclinical cancer models.

Squires M, Ward G, Saxty G, Berdini V, Cleasby A, King P, Angibaud P, Perera T, Fazal L, Ross D, Jones CG, Madin A, Benning RK, Vickerstaffe E, O'Brien A, Frederickson M, Reader M, Hamlett C, Batey MA, Rich S, Carr M, Miller D, Feltell R, Thiru A, Bethell S, Devine LA, Graham BL, Pike A, Cosme J, Lewis EJ, Freyne E, Lyons J, Irving J, Murray C, Newell DR, Thompson NT.

Mol Cancer Ther. 2011 Sep;10(9):1542-52. doi: 10.1158/1535-7163.MCT-11-0426. Epub 2011 Jul 15.

5.

Identification of a series of substituted 2-piperazinyl-5-pyrimidylhydroxamic acids as potent histone deacetylase inhibitors.

Angibaud P, Van Emelen K, Decrane L, van Brandt S, Ten Holte P, Pilatte I, Roux B, Poncelet V, Speybrouck D, Queguiner L, Gaurrand S, Mariën A, Floren W, Janssen L, Verdonck M, van Dun J, van Gompel J, Gilissen R, Mackie C, Du Jardin M, Peeters J, Noppe M, Van Hijfte L, Freyne E, Page M, Janicot M, Arts J.

Bioorg Med Chem Lett. 2010 Jan 1;20(1):294-8. doi: 10.1016/j.bmcl.2009.10.118. Epub 2009 Oct 30.

PMID:
19906529
6.

Design and synthesis of a series of piperazine-1-carboxamidine derivatives with antifungal activity resulting from accumulation of endogenous reactive oxygen species.

François IE, Thevissen K, Pellens K, Meert EM, Heeres J, Freyne E, Coesemans E, Viellevoye M, Deroose F, Martinez Gonzalez S, Pastor J, Corens D, Meerpoel L, Borgers M, Ausma J, Dispersyn GD, Cammue BP.

ChemMedChem. 2009 Oct;4(10):1714-21. doi: 10.1002/cmdc.200900249.

PMID:
19705386
7.

Discovery of pyrimidyl-5-hydroxamic acids as new potent histone deacetylase inhibitors.

Angibaud P, Arts J, Van Emelen K, Poncelet V, Pilatte I, Roux B, Van Brandt S, Verdonck M, De Winter H, Ten Holte P, Marien A, Floren W, Janssens B, Van Dun J, Aerts A, Van Gompel J, Gaurrand S, Queguiner L, Argoullon JM, Van Hijfte L, Freyne E, Janicot M.

Eur J Med Chem. 2005 Jun;40(6):597-606. Epub 2005 Mar 3.

PMID:
15922843
8.

Synthesis and biological evaluation of 1,2,4-triazinylphenylalkylthiazolecarboxylic acid esters as cytokine-inhibiting antedrugs with strong bronchodilating effects in an animal model of asthma.

Freyne EJ, Lacrampe JF, Deroose F, Boeckx GM, Willems M, Embrechts W, Coesemans E, Willems JJ, Fortin JM, Ligney Y, Dillen LL, Cools WF, Goossens J, Corens D, De Groot A, Van Wauwe JP.

J Med Chem. 2005 Mar 24;48(6):2167-75.

PMID:
15771459
9.

Substituted azoloquinolines and -quinazolines as new potent farnesyl protein transferase inhibitors.

Angibaud P, Bourdrez X, End DW, Freyne E, Janicot M, Lezouret P, Ligny Y, Mannens G, Damsch S, Mevellec L, Meyer C, Muller P, Pilatte I, Poncelet V, Roux B, Smets G, Van Dun J, Van Remoortere P, Venet M, Wouters W.

Bioorg Med Chem Lett. 2003 Dec 15;13(24):4365-9.

PMID:
14643327
10.

4-methyl-1,2,4-triazol-3-yl heterocycle as an alternative to the 1-methylimidazol-5-yl moiety in the farnesyltransferase inhibitor ZARNESTRA.

Angibaud P, Saha AK, Bourdrez X, End DW, Freyne E, Lezouret P, Mannens G, Mevellec L, Meyer C, Pilatte I, Poncelet V, Roux B, Smets G, Van Dun J, Venet M, Wouters W.

Bioorg Med Chem Lett. 2003 Dec 15;13(24):4361-4.

PMID:
14643326
11.

5-imidazolyl-quinolinones, -quinazolinones and -benzo-azepinones as farnesyltransferase inhibitors.

Angibaud P, Bourdrez X, Devine A, End DW, Freyne E, Ligny Y, Muller P, Mannens G, Pilatte I, Poncelet V, Skrzat S, Smets G, Van Dun J, Van Remoortere P, Venet M, Wouters W.

Bioorg Med Chem Lett. 2003 May 5;13(9):1543-7.

PMID:
12699751
12.

Synthesis and biological evaluation of imidazol-2-one and 2-cyanoiminoimidazole derivatives: novel series of PDE4 inhibitors.

Andrés JI, Alonso JM, Díaz A, Fernández J, Iturrino L, Martínez P, Matesanz E, Freyne EJ, Deroose F, Boeckx G, Petit D, Diels G, Megens A, Somers M, Van Wauwe J, Stoppie P, Cools M, De Clerck F, Peeters D, de Chaffoy D.

Bioorg Med Chem Lett. 2002 Feb 25;12(4):653-8.

PMID:
11844693
13.

Identification of R146225 as a novel, orally active inhibitor of interleukin-5 biosynthesis.

Van Wauwe J, Aerts F, Cools M, Deroose F, Freyne E, Goossens J, Hermans B, Lacrampe J, Van Genechten H, Van Gerven F, Van Nyen G.

J Pharmacol Exp Ther. 2000 Nov;295(2):655-61.

PMID:
11046102
14.

Synthesis of LIAZAL, a retinoic acid metabolism blocking agent (RAMBA) with potential clinical applications in oncology and dermatology.

Freyne E, Raeymaekers A, Venet M, Sanz G, Wouters W, De Coster R, Wauwe JV.

Bioorg Med Chem Lett. 1998 Feb 3;8(3):267-72.

PMID:
9871667
15.
16.

Cardiac and hemodynamic effects of intravenous R 80122, a new phosphodiesterase III inhibitor, in anesthetized and awake dogs.

Van de Water A, d'Aubioul J, Van Gerven W, de Chaffoy de Courcelles D, Freyne E, Xhonneux R, Reneman RS, Janssen PA.

Arch Int Pharmacodyn Ther. 1992 Mar-Apr;316:60-74.

PMID:
1530374
17.

Comparative effects of the aromatase inhibitor R76713 and of its enantiomers R83839 and R83842 on steroid biosynthesis in vitro and in vivo.

Wouters W, De Coster R, van Dun J, Krekels MD, Dillen A, Raeymaekers A, Freyne E, Van Gelder J, Sanz G, Venet M, et al.

J Steroid Biochem Mol Biol. 1990 Dec 20;37(6):1049-54.

PMID:
2178362
18.

R 75251, a new inhibitor of steroid biosynthesis.

Bruynseels J, De Coster R, Van Rooy P, Wouters W, Coene MC, Snoeck E, Raeymaekers A, Freyne E, Sanz G, Vanden Bussche G, et al.

Prostate. 1990;16(4):345-57.

PMID:
2164659
19.

R 76713, a new specific non-steroidal aromatase inhibitor.

Wouters W, De Coster R, Krekels M, van Dun J, Beerens D, Haelterman C, Raeymaekers A, Freyne E, Van Gelder J, Venet M, et al.

J Steroid Biochem. 1989 Jun;32(6):781-8.

PMID:
2755126
20.

R 68 070: thromboxane A2 synthetase inhibition and thromboxane A2/prostaglandin endoperoxide receptor blockade combined in one molecule--I. Biochemical profile in vitro.

De Clerck F, Beetens J, de Chaffoy de Courcelles D, Freyne E, Janssen PA.

Thromb Haemost. 1989 Feb 28;61(1):35-42.

PMID:
2546278
21.

R 68 070: thromboxane A2 synthetase inhibition and thromboxane A2/prostaglandin endoperoxide receptor blockade, combined in one molecule.

De Clerck F, Beetens J, de Chaffoy de Courcelles D, Vercammen E, Freyne E, Janssen PA.

Prog Clin Biol Res. 1989;301:567-72. No abstract available.

PMID:
2529556

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