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RP-3500: A Novel, Potent, and Selective ATR Inhibitor that is Effective in Preclinical Models as a Monotherapy and in Combination with PARP Inhibitors.
Roulston A, Zimmermann M, Papp R, Skeldon A, Pellerin C, Dumas-Bérube É, Dumais V, Dorich S, Fader LD, Fournier S, Li L, Leclaire ME, Yin SY, Chefson A, Alam H, Yang W, Fugère-Desjardins C, Vignini-Hammond S, Skorey K, Mulani A, Rimkunas V, Veloso A, Hamel M, Stocco R, Mamane Y, Li Z, Young JTF, Zinda M, Black WC. Roulston A, et al. Among authors: hamel m. Mol Cancer Ther. 2022 Feb;21(2):245-256. doi: 10.1158/1535-7163.MCT-21-0615. Epub 2021 Dec 15. Mol Cancer Ther. 2022. PMID: 34911817 Free PMC article.
Applying the pro-drug approach to afford highly bioavailable antagonists of P2Y(14).
Robichaud J, Fournier JF, Gagné S, Gauthier JY, Hamel M, Han Y, Hénault M, Kargman S, Levesque JF, Mamane Y, Mancini J, Morin N, Mulrooney E, Wu J, Black WC. Robichaud J, et al. Among authors: hamel m. Bioorg Med Chem Lett. 2011 Jul 15;21(14):4366-8. doi: 10.1016/j.bmcl.2010.12.113. Epub 2010 Dec 28. Bioorg Med Chem Lett. 2011. PMID: 21689930
Identification of RP-6685, an Orally Bioavailable Compound that Inhibits the DNA Polymerase Activity of Polθ.
Bubenik M, Mader P, Mochirian P, Vallée F, Clark J, Truchon JF, Perryman AL, Pau V, Kurinov I, Zahn KE, Leclaire ME, Papp R, Mathieu MC, Hamel M, Duffy NM, Godbout C, Casas-Selves M, Falgueyret JP, Baruah PS, Nicolas O, Stocco R, Poirier H, Martino G, Fortin AB, Roulston A, Chefson A, Dorich S, St-Onge M, Patel P, Pellerin C, Ciblat S, Pinter T, Barabé F, El Bakkouri M, Parikh P, Gervais C, Sfeir A, Mamane Y, Morris SJ, Black WC, Sicheri F, Gallant M. Bubenik M, et al. Among authors: hamel m. J Med Chem. 2022 Oct 13;65(19):13198-13215. doi: 10.1021/acs.jmedchem.2c00998. Epub 2022 Sep 20. J Med Chem. 2022. PMID: 36126059 Free PMC article.
Discovery of the Potent and Selective ATR Inhibitor Camonsertib (RP-3500).
Black WC, Abdoli A, An X, Auger A, Beaulieu P, Bernatchez M, Caron C, Chefson A, Crane S, Diallo M, Dorich S, Fader LD, Ferraro GB, Fournier S, Gao Q, Ginzburg Y, Hamel M, Han Y, Jones P, Lanoix S, Lacbay CM, Leclaire ME, Levy M, Mamane Y, Mulani A, Papp R, Pellerin C, Picard A, Skeldon A, Skorey K, Stocco R, St-Onge M, Truchon JF, Truong VL, Zimmermann M, Zinda M, Roulston A. Black WC, et al. Among authors: hamel m. J Med Chem. 2024 Feb 22;67(4):2349-2368. doi: 10.1021/acs.jmedchem.3c01917. Epub 2024 Feb 1. J Med Chem. 2024. PMID: 38299539
Pharmacological characterization of MK-7246, a potent and selective CRTH2 (chemoattractant receptor-homologous molecule expressed on T-helper type 2 cells) antagonist.
Gervais FG, Sawyer N, Stocco R, Hamel M, Krawczyk C, Sillaots S, Denis D, Wong E, Wang Z, Gallant M, Abraham WM, Slipetz D, Crackower MA, O'Neill GP. Gervais FG, et al. Among authors: hamel m. Mol Pharmacol. 2011 Jan;79(1):69-76. doi: 10.1124/mol.110.068585. Epub 2010 Oct 13. Mol Pharmacol. 2011. PMID: 20943773
The identification of 4,7-disubstituted naphthoic acid derivatives as UDP-competitive antagonists of P2Y14.
Gauthier JY, Belley M, Deschênes D, Fournier JF, Gagné S, Gareau Y, Hamel M, Hénault M, Hyjazie H, Kargman S, Lavallée G, Levesque JF, Li L, Mamane Y, Mancini J, Morin N, Mulrooney E, Robichaud J, Thérien M, Tranmer G, Wang Z, Wu J, Black WC. Gauthier JY, et al. Among authors: hamel m. Bioorg Med Chem Lett. 2011 May 15;21(10):2836-9. doi: 10.1016/j.bmcl.2011.03.081. Epub 2011 Mar 31. Bioorg Med Chem Lett. 2011. PMID: 21507640
Synthesis and SAR of pyrimidine-based, non-nucleotide P2Y14 receptor antagonists.
Guay D, Beaulieu C, Belley M, Crane SN, DeLuca J, Gareau Y, Hamel M, Henault M, Hyjazie H, Kargman S, Chan CC, Xu L, Gordon R, Li L, Mamane Y, Morin N, Mancini J, Thérien M, Tranmer G, Truong VL, Wang Z, Black WC. Guay D, et al. Among authors: hamel m. Bioorg Med Chem Lett. 2011 May 15;21(10):2832-5. doi: 10.1016/j.bmcl.2011.03.084. Epub 2011 Mar 30. Bioorg Med Chem Lett. 2011. PMID: 21507642
Azaindoles as potent CRTH2 receptor antagonists.
Simard D, Leblanc Y, Berthelette C, Zaghdane MH, Molinaro C, Wang Z, Gallant M, Lau S, Thao T, Hamel M, Stocco R, Sawyer N, Sillaots S, Gervais F, Houle R, Lévesque JF. Simard D, et al. Among authors: hamel m. Bioorg Med Chem Lett. 2011 Jan 15;21(2):841-5. doi: 10.1016/j.bmcl.2010.11.084. Epub 2010 Nov 21. Bioorg Med Chem Lett. 2011. PMID: 21185722
New indole amide derivatives as potent CRTH2 receptor antagonists.
Zaghdane H, Boyd M, Colucci J, Simard D, Berthelette C, Leblanc Y, Wang Z, Houle R, Lévesque JF, Molinaro C, Hamel M, Stocco R, Sawyer N, Sillaots S, Gervais F, Gallant M. Zaghdane H, et al. Among authors: hamel m. Bioorg Med Chem Lett. 2011 Jun 1;21(11):3471-4. doi: 10.1016/j.bmcl.2011.03.085. Epub 2011 Mar 30. Bioorg Med Chem Lett. 2011. PMID: 21515053
446 results