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Items: 1 to 20 of 128

1.

p38 MAP kinase inhibitors. Part 3: SAR on 3,4-dihydropyrimido[4,5-d]pyrimidin-2-ones and 3,4-dihydropyrido[4,3-d]pyrimidin-2-ones.

Natarajan SR, Wisnoski DD, Thompson JE, O'Neill EA, O'Keefe SJ.

Bioorg Med Chem Lett. 2006 Aug 15;16(16):4400-4. Epub 2006 Jun 5.

PMID:
16750629
2.

P38 MAP kinase inhibitors: evolution of imidazole-based and pyrido-pyrimidin-2-one lead classes.

Natarajan SR, Doherty JB.

Curr Top Med Chem. 2005;5(10):987-1003. Review.

PMID:
16178742
3.

p38 MAP kinase inhibitors. Part 6: 2-arylpyridazin-3-ones as templates for inhibitor design.

Natarajan SR, Heller ST, Nam K, Singh SB, Scapin G, Patel S, Thompson JE, Fitzgerald CE, O'Keefe SJ.

Bioorg Med Chem Lett. 2006 Nov 15;16(22):5809-13. Epub 2006 Aug 30.

PMID:
16945533
4.

Structure-activity relationships of 6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)pyrido[2,3-d]pyrimidin-7-ones: toward selective Abl inhibitors.

Antczak C, Veach DR, Ramirez CN, Minchenko MA, Shum D, Calder PA, Frattini MG, Clarkson B, Djaballah H.

Bioorg Med Chem Lett. 2009 Dec 15;19(24):6872-6. doi: 10.1016/j.bmcl.2009.10.085. Epub 2009 Oct 23.

5.

The development of novel 1,2-dihydro-pyrimido[4,5-c]pyridazine based inhibitors of lymphocyte specific kinase (Lck).

Sabat M, Vanrens JC, Brugel TA, Maier J, Laufersweiler MJ, Golebiowski A, De B, Easwaran V, Hsieh LC, Rosegen J, Berberich S, Suchanek E, Janusz MJ.

Bioorg Med Chem Lett. 2006 Aug 15;16(16):4257-61. Epub 2006 Jun 6.

PMID:
16757169
6.

Structure-activity relationships of triazolopyridine oxazole p38 inhibitors: identification of candidates for clinical development.

McClure KF, Letavic MA, Kalgutkar AS, Gabel CA, Audoly L, Barberia JT, Braganza JF, Carter D, Carty TJ, Cortina SR, Dombroski MA, Donahue KM, Elliott NC, Gibbons CP, Jordan CK, Kuperman AV, Labasi JM, Laliberte RE, McCoy JM, Naiman BM, Nelson KL, Nguyen HT, Peese KM, Sweeney FJ, Taylor TJ, Trebino CE, Abramov YA, Laird ER, Volberg WA, Zhou J, Bach J, Lombardo F.

Bioorg Med Chem Lett. 2006 Aug 15;16(16):4339-44. Epub 2006 Jun 12.

PMID:
16759861
7.

SAR of 3,4-dihydropyrido[3,2-d]pyrimidone p38 inhibitors.

Liu L, Stelmach JE, Natarajan SR, Chen MH, Singh SB, Schwartz CD, Fitzgerald CE, O'Keefe SJ, Zaller DM, Schmatz DM, Doherty JB.

Bioorg Med Chem Lett. 2003 Nov 17;13(22):3979-82.

PMID:
14592489
8.

Design, synthesis and activity of a potent, selective series of N-aryl pyridinone inhibitors of p38 kinase.

Selness SR, Boehm TL, Walker JK, Devadas B, Durley RC, Kurumbail R, Shieh H, Xing L, Hepperle M, Rucker PV, Jerome KD, Benson AG, Marrufo LD, Madsen HM, Hitchcock J, Owen TJ, Christie L, Promo MA, Hickory BS, Alvira E, Naing W, Blevis-Bal R, Devraj RV, Messing D, Schindler JF, Hirsch J, Saabye M, Bonar S, Webb E, Anderson G, Monahan JB.

Bioorg Med Chem Lett. 2011 Jul 1;21(13):4059-65. doi: 10.1016/j.bmcl.2011.04.120. Epub 2011 May 13.

PMID:
21640588
9.

p38MAP kinase inhibitors. Part 1: design and development of a new class of potent and highly selective inhibitors based on 3,4-dihydropyrido[3,2-d]pyrimidone scaffold.

Natarajan SR, Wisnoski DD, Singh SB, Stelmach JE, O'Neill EA, Schwartz CD, Thompson CM, Fitzgerald CE, O'Keefe SJ, Kumar S, Hop CE, Zaller DM, Schmatz DM, Doherty JB.

Bioorg Med Chem Lett. 2003 Jan 20;13(2):273-6.

PMID:
12482438
10.

Synthesis and biological evaluation of trisubstituted imidazole derivatives as inhibitors of p38alpha mitogen-activated protein kinase.

Kim DK, Lim JH, Lee JA, Dewang PM.

Bioorg Med Chem Lett. 2008 Jul 15;18(14):4006-10. doi: 10.1016/j.bmcl.2008.06.007. Epub 2008 Jun 6.

PMID:
18571921
11.

Synthesis of highly substituted 2,3-dihydropyrimido[4,5-d]pyrimidin-4(1H)-ones from 4,6-dichloro-5-formylpyrimidine, amines and aldehydes.

Xiang J, Geng C, Yi L, Dang Q, Bai X.

Mol Divers. 2011 Nov;15(4):839-47. doi: 10.1007/s11030-011-9314-5. Epub 2011 Apr 21.

PMID:
21509500
12.

Synthesis of 4-substituted pyrido[2,3-d]pyrimidin-4(1H)-one as analgesic and anti-inflammatory agents.

El-Gazzar AR, Hafez HN.

Bioorg Med Chem Lett. 2009 Jul 1;19(13):3392-7. doi: 10.1016/j.bmcl.2009.05.044. Epub 2009 May 18.

PMID:
19481936
13.

Structural basis for p38alpha MAP kinase quinazolinone and pyridol-pyrimidine inhibitor specificity.

Fitzgerald CE, Patel SB, Becker JW, Cameron PM, Zaller D, Pikounis VB, O'Keefe SJ, Scapin G.

Nat Struct Biol. 2003 Sep;10(9):764-9. Epub 2003 Aug 3.

PMID:
12897767
14.

The identification of pyrazolo[1,5-a]pyridines as potent p38 kinase inhibitors.

Cheung M, Harris PA, Badiang JG, Peckham GE, Chamberlain SD, Alberti MJ, Jung DK, Harris SS, Bramson NH, Epperly AH, Stimpson SA, Peel MR.

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5428-30. doi: 10.1016/j.bmcl.2008.09.040. Epub 2008 Sep 12.

PMID:
18818075
15.

Design and synthesis of potent pyridazine inhibitors of p38 MAP kinase.

Tamayo N, Liao L, Goldberg M, Powers D, Tudor YY, Yu V, Wong LM, Henkle B, Middleton S, Syed R, Harvey T, Jang G, Hungate R, Dominguez C.

Bioorg Med Chem Lett. 2005 May 2;15(9):2409-13.

PMID:
15837335
16.

'Reverse' alpha-ketoamide-based p38 MAP kinase inhibitors.

Montalban AG, Boman E, Chang CD, Ceide SC, Dahl R, Dalesandro D, Delaet NG, Erb E, Gibbs A, Kahl J, Kessler L, Lundström J, Miller S, Nakanishi H, Roberts E, Saiah E, Sullivan R, Wang Z, Larson CJ.

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5456-9. doi: 10.1016/j.bmcl.2008.09.028. Epub 2008 Sep 11.

PMID:
18835164
17.

Synthesis and biological activity of quinolinone and dihydroquinolinone p38 MAP kinase inhibitors.

Chen MH, Fitzgerald P, Singh SB, O'Neill EA, Schwartz CD, Thompson CM, O'Keefe SJ, Zaller DM, Doherty JB.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):2222-6. doi: 10.1016/j.bmcl.2006.10.097. Epub 2006 Nov 6.

PMID:
18316187
18.

Chemical proteomic analysis reveals alternative modes of action for pyrido[2,3-d]pyrimidine kinase inhibitors.

Wissing J, Godl K, Brehmer D, Blencke S, Weber M, Habenberger P, Stein-Gerlach M, Missio A, Cotten M, Müller S, Daub H.

Mol Cell Proteomics. 2004 Dec;3(12):1181-93. Epub 2004 Oct 8.

19.

Development of 2-aryl substituted quinazolin-4(3H)-one, pyrido[4,3-d]pyrimidin-4(3H)-one and pyrido[2,3-d]pyrimidin-4(3H)-one derivatives as microsomal prostaglandin E(2) synthase-1 inhibitors.

Banerjee A, Pawar MY, Patil S, Yadav PS, Kadam PA, Kattige VG, Deshpande DS, Pednekar PV, Pisat MK, Gharat LA.

Bioorg Med Chem Lett. 2014 Oct 15;24(20):4838-44. doi: 10.1016/j.bmcl.2014.08.056. Epub 2014 Sep 2.

PMID:
25260492
20.

C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays.

Le Bihan YV, Lanigan RM, Atrash B, McLaughlin MG, Velupillai S, Malcolm AG, England KS, Ruda GF, Mok NY, Tumber A, Tomlin K, Saville H, Shehu E, McAndrew C, Carmichael L, Bennett JM, Jeganathan F, Eve P, Donovan A, Hayes A, Wood F, Raynaud FI, Fedorov O, Brennan PE, Burke R, van Montfort RLM, Rossanese OW, Blagg J, Bavetsias V.

Eur J Med Chem. 2019 Sep 1;177:316-337. doi: 10.1016/j.ejmech.2019.05.041. Epub 2019 May 17.

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