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Items: 25

1.

Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma.

Fournier JF, Bhurruth-Alcor Y, Musicki B, Aubert J, Aurelly M, Bouix-Peter C, Bouquet K, Chantalat L, Delorme M, Drean B, Duvert G, Fleury-Bregeot N, Gauthier B, Grisendi K, Harris CS, Hennequin LF, Isabet T, Joly F, Lafitte G, Millois C, Morgentin R, Pascau J, Piwnica D, Rival Y, Soulet C, Thoreau É, Tomas L.

Bioorg Med Chem Lett. 2018 Sep 15;28(17):2985-2992. doi: 10.1016/j.bmcl.2018.06.029. Epub 2018 Jun 18.

PMID:
30122227
2.

Rational Drug Design of Topically Administered Caspase 1 Inhibitors for the Treatment of Inflammatory Acne.

Fournier JF, Clary L, Chambon S, Dumais L, Harris CS, Millois C, Pierre R, Talano S, Thoreau É, Aubert J, Aurelly M, Bouix-Peter C, Brethon A, Chantalat L, Christin O, Comino C, El-Bazbouz G, Ghilini AL, Isabet T, Lardy C, Luzy AP, Mathieu C, Mebrouk K, Orfila D, Pascau J, Reverse K, Roche D, Rodeschini V, Hennequin LF.

J Med Chem. 2018 May 10;61(9):4030-4051. doi: 10.1021/acs.jmedchem.8b00067. Epub 2018 Apr 24.

PMID:
29648825
3.

Sulfoximines as potent RORγ inverse agonists.

Ouvry G, Bihl F, Bouix-Peter C, Christin O, Defoin-Platel C, Deret S, Feret C, Froude D, Hacini-Rachinel F, Harris CS, Hervouet C, Lafitte G, Luzy AP, Musicki B, Orfila D, Parnet V, Pascau C, Pascau J, Pierre R, Raffin C, Rossio P, Spiesse D, Taquet N, Thoreau E, Vatinel R, Vial E, Hennequin LF.

Bioorg Med Chem Lett. 2018 May 1;28(8):1269-1273. doi: 10.1016/j.bmcl.2018.03.041. Epub 2018 Mar 17.

PMID:
29571573
4.

Discovery and Characterization of CD12681, a Potent RORγ Inverse Agonist, Preclinical Candidate for the Topical Treatment of Psoriasis.

Ouvry G, Atrux-Tallau N, Bihl F, Bondu A, Bouix-Peter C, Carlavan I, Christin O, Cuadrado MJ, Defoin-Platel C, Deret S, Duvert D, Feret C, Forissier M, Fournier JF, Froude D, Hacini-Rachinel F, Harris CS, Hervouet C, Huguet H, Lafitte G, Luzy AP, Musicki B, Orfila D, Ozello B, Pascau C, Pascau J, Parnet V, Peluchon G, Pierre R, Piwnica D, Raffin C, Rossio P, Spiesse D, Taquet N, Thoreau E, Vatinel R, Vial E, Hennequin LF.

ChemMedChem. 2018 Feb 20;13(4):321-337. doi: 10.1002/cmdc.201700758. Epub 2018 Feb 6.

PMID:
29327456
5.

Discovery and process development of a novel TACE inhibitor for the topical treatment of psoriasis.

Boiteau JG, Ouvry G, Arlabosse JM, Astri S, Beillard A, Bhurruth-Alcor Y, Bonnary L, Bouix-Peter C, Bouquet K, Bourotte M, Cardinaud I, Comino C, Deprez B, Duvert D, Féret A, Hacini-Rachinel F, Harris CS, Luzy AP, Mathieu A, Millois C, Orsini N, Pascau J, Pinto A, Piwnica D, Polge G, Reitz A, Reversé K, Rodeville N, Rossio P, Spiesse D, Tabet S, Taquet N, Tomas L, Vial E, Hennequin LF.

Bioorg Med Chem. 2018 Feb 15;26(4):945-956. doi: 10.1016/j.bmc.2017.07.054. Epub 2017 Aug 2.

PMID:
28818461
6.

Identification of novel TACE inhibitors compatible with topical application.

Ouvry G, Berton Y, Bhurruth-Alcor Y, Bonnary L, Bouix-Peter C, Bouquet K, Bourotte M, Chambon S, Comino C, Deprez B, Duvert D, Duvert G, Hacini-Rachinel F, Harris CS, Luzy AP, Mathieu A, Millois C, Pascau J, Pinto A, Polge G, Reitz A, Reversé K, Rosignoli C, Taquet N, Hennequin LF.

Bioorg Med Chem Lett. 2017 Apr 15;27(8):1848-1853. doi: 10.1016/j.bmcl.2017.02.035. Epub 2017 Feb 20.

PMID:
28274635
7.

Discovery of phenoxyindazoles and phenylthioindazoles as RORγ inverse agonists.

Ouvry G, Bouix-Peter C, Ciesielski F, Chantalat L, Christin O, Comino C, Duvert D, Feret C, Harris CS, Lamy L, Luzy AP, Musicki B, Orfila D, Pascau J, Parnet V, Perrin A, Pierre R, Polge G, Raffin C, Rival Y, Taquet N, Thoreau E, Hennequin LF.

Bioorg Med Chem Lett. 2016 Dec 1;26(23):5802-5808. doi: 10.1016/j.bmcl.2016.10.023. Epub 2016 Oct 12.

PMID:
27815118
8.

Discovery of AZD8931, an Equipotent, Reversible Inhibitor of Signaling by EGFR, HER2, and HER3 Receptors.

Barlaam B, Anderton J, Ballard P, Bradbury RH, Hennequin LF, Hickinson DM, Kettle JG, Kirk G, Klinowska T, Lambert-van der Brempt C, Trigwell C, Vincent J, Ogilvie D.

ACS Med Chem Lett. 2013 May 31;4(8):742-6. doi: 10.1021/ml400146c. eCollection 2013 Aug 8.

9.

Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530.

Green TP, Fennell M, Whittaker R, Curwen J, Jacobs V, Allen J, Logie A, Hargreaves J, Hickinson DM, Wilkinson RW, Elvin P, Boyer B, Carragher N, Plé PA, Bermingham A, Holdgate GA, Ward WH, Hennequin LF, Davies BR, Costello GF.

Mol Oncol. 2009 Jun;3(3):248-61. doi: 10.1016/j.molonc.2009.01.002. Epub 2009 Feb 7.

10.

Neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.

Ballard P, Barlaam BC, Bradbury RH, Dishington A, Hennequin LF, Hickinson DM, Hollingsworth IM, Kettle JG, Klinowska T, Ogilvie DJ, Pearson SE, Scott JS, Suleman A, Whittaker R, Williams EJ, Wood R, Wright L.

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6326-9. Epub 2007 Sep 2.

PMID:
17869514
11.

N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.

Hennequin LF, Allen J, Breed J, Curwen J, Fennell M, Green TP, Lambert-van der Brempt C, Morgentin R, Norman RA, Olivier A, Otterbein L, Plé PA, Warin N, Costello G.

J Med Chem. 2006 Nov 2;49(22):6465-88.

PMID:
17064066
12.

Inhibitors of epidermal growth factor receptor tyrosine kinase: optimisation of potency and in vivo pharmacokinetics.

Ballard P, Bradbury RH, Harris CS, Hennequin LF, Hickinson M, Kettle JG, Kendrew J, Klinowska T, Ogilvie DJ, Pearson SE, Williams EJ, Wilson I.

Bioorg Med Chem Lett. 2006 Sep 15;16(18):4908-12. Epub 2006 Jun 27.

PMID:
16806916
13.

Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: synthesis and structure-activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors.

Hennequin LF, Ballard P, Boyle FT, Delouvrié B, Ellston RP, Halsall CT, Harris CS, Hudson K, Kendrew J, Pease JE, Ross HS, Smith P, Vincent JL.

Bioorg Med Chem Lett. 2006 May 15;16(10):2672-6. Epub 2006 Mar 3.

PMID:
16516473
14.

Inhibitors of epidermal growth factor receptor tyrosine kinase: Novel C-5 substituted anilinoquinazolines designed to target the ribose pocket.

Ballard P, Bradbury RH, Harris CS, Hennequin LF, Hickinson M, Johnson PD, Kettle JG, Klinowska T, Leach AG, Morgentin R, Pass M, Ogilvie DJ, Olivier A, Warin N, Williams EJ.

Bioorg Med Chem Lett. 2006 Mar 15;16(6):1633-7. Epub 2005 Dec 27.

PMID:
16380259
15.

5-Substituted 4-anilinoquinazolines as potent, selective and orally active inhibitors of erbB2 receptor tyrosine kinase.

Ballard P, Bradbury RH, Hennequin LF, Hickinson DM, Johnson PD, Kettle JG, Klinowska T, Morgentin R, Ogilvie DJ, Olivier A.

Bioorg Med Chem Lett. 2005 Oct 1;15(19):4226-9.

PMID:
16055332
16.

AZD2171: a highly potent, orally bioavailable, vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for the treatment of cancer.

Wedge SR, Kendrew J, Hennequin LF, Valentine PJ, Barry ST, Brave SR, Smith NR, James NH, Dukes M, Curwen JO, Chester R, Jackson JA, Boffey SJ, Kilburn LL, Barnett S, Richmond GH, Wadsworth PF, Walker M, Bigley AL, Taylor ST, Cooper L, Beck S, Jürgensmeier JM, Ogilvie DJ.

Cancer Res. 2005 May 15;65(10):4389-400.

17.

Discovery of a new class of anilinoquinazoline inhibitors with high affinity and specificity for the tyrosine kinase domain of c-Src.

Plé PA, Green TP, Hennequin LF, Curwen J, Fennell M, Allen J, Lambert-Van Der Brempt C, Costello G.

J Med Chem. 2004 Feb 12;47(4):871-87.

PMID:
14761189
18.

ZM323881, a novel inhibitor of vascular endothelial growth factor-receptor-2 tyrosine kinase activity.

Whittles CE, Pocock TM, Wedge SR, Kendrew J, Hennequin LF, Harper SJ, Bates DO.

Microcirculation. 2002 Dec;9(6):513-22.

PMID:
12483548
19.

ZD6474 inhibits vascular endothelial growth factor signaling, angiogenesis, and tumor growth following oral administration.

Wedge SR, Ogilvie DJ, Dukes M, Kendrew J, Chester R, Jackson JA, Boffey SJ, Valentine PJ, Curwen JO, Musgrove HL, Graham GA, Hughes GD, Thomas AP, Stokes ES, Curry B, Richmond GH, Wadsworth PF, Bigley AL, Hennequin LF.

Cancer Res. 2002 Aug 15;62(16):4645-55.

20.

Novel 4-anilinoquinazolines with C-7 basic side chains: design and structure activity relationship of a series of potent, orally active, VEGF receptor tyrosine kinase inhibitors.

Hennequin LF, Stokes ES, Thomas AP, Johnstone C, Plé PA, Ogilvie DJ, Dukes M, Wedge SR, Kendrew J, Curwen JO.

J Med Chem. 2002 Mar 14;45(6):1300-12.

PMID:
11881999
21.

ZD4190: an orally active inhibitor of vascular endothelial growth factor signaling with broad-spectrum antitumor efficacy.

Wedge SR, Ogilvie DJ, Dukes M, Kendrew J, Curwen JO, Hennequin LF, Thomas AP, Stokes ES, Curry B, Richmond GH, Wadsworth PF.

Cancer Res. 2000 Feb 15;60(4):970-5.

22.

Design and structure-activity relationship of a new class of potent VEGF receptor tyrosine kinase inhibitors.

Hennequin LF, Thomas AP, Johnstone C, Stokes ES, Plé PA, Lohmann JJ, Ogilvie DJ, Dukes M, Wedge SR, Curwen JO, Kendrew J, Lambert-van der Brempt C.

J Med Chem. 1999 Dec 30;42(26):5369-89.

PMID:
10639280
23.

Design and synthesis of potent non-polyglutamatable quinazoline antifolate thymidylate synthase inhibitors.

Marsham PR, Wardleworth JM, Boyle FT, Hennequin LF, Kimbell R, Brown M, Jackman AL.

J Med Chem. 1999 Sep 23;42(19):3809-20.

PMID:
10508430
24.

Quinazoline antifolates thymidylate synthase inhibitors: lipophilic analogues with modification to the C2-methyl substituent.

Hennequin LF, Boyle FT, Wardleworth JM, Marsham PR, Kimbell R, Jackman AL.

J Med Chem. 1996 Feb 2;39(3):695-704.

PMID:
8576912
25.

Synthesis and biological activity of C-3' ortho dihydroxyphthalimido cephalosporins.

Baudart MG, Hennequin LF.

J Antibiot (Tokyo). 1993 Sep;46(9):1458-70.

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