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Items: 1 to 20 of 100

1.

Synthesis and evaluation of carbamoylmethylene linked prodrugs of BMS-582949, a clinical p38α inhibitor.

Liu C, Lin J, Everlof G, Gesenberg C, Zhang H, Marathe PH, Malley M, Galella MA, McKinnon M, Dodd JH, Barrish JC, Schieven GL, Leftheris K.

Bioorg Med Chem Lett. 2013 May 15;23(10):3028-33. doi: 10.1016/j.bmcl.2013.03.022. Epub 2013 Mar 15.

PMID:
23578688
2.

Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor.

Liu C, Lin J, Hynes J, Wu H, Wrobleski ST, Lin S, Dhar TG, Vrudhula VM, Sun JH, Chao S, Zhao R, Wang B, Chen BC, Everlof G, Gesenberg C, Zhang H, Marathe PH, McIntyre KW, Taylor TL, Gillooly K, Shuster DJ, McKinnon M, Dodd JH, Barrish JC, Schieven GL, Leftheris K.

J Med Chem. 2015 Oct 8;58(19):7775-84. doi: 10.1021/acs.jmedchem.5b00839. Epub 2015 Sep 22.

PMID:
26359680
3.

Discovery of brivanib alaninate ((S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), a novel prodrug of dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 kinase inhibitor (BMS-540215).

Cai ZW, Zhang Y, Borzilleri RM, Qian L, Barbosa S, Wei D, Zheng X, Wu L, Fan J, Shi Z, Wautlet BS, Mortillo S, Jeyaseelan R Sr, Kukral DW, Kamath A, Marathe P, D'Arienzo C, Derbin G, Barrish JC, Robl JA, Hunt JT, Lombardo LJ, Fargnoli J, Bhide RS.

J Med Chem. 2008 Mar 27;51(6):1976-80. doi: 10.1021/jm7013309. Epub 2008 Feb 21.

PMID:
18288793
4.

Synthesis and SAR of new pyrrolo[2,1-f][1,2,4]triazines as potent p38 alpha MAP kinase inhibitors.

Wrobleski ST, Lin S, Hynes J Jr, Wu H, Pitt S, Shen DR, Zhang R, Gillooly KM, Shuster DJ, McIntyre KW, Doweyko AM, Kish KF, Tredup JA, Duke GJ, Sack JS, McKinnon M, Dodd J, Barrish JC, Schieven GL, Leftheris K.

Bioorg Med Chem Lett. 2008 Apr 15;18(8):2739-44. doi: 10.1016/j.bmcl.2008.02.067. Epub 2008 Mar 4.

PMID:
18364256
5.

Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 2. Synthesis and characterization of a novel imide-type prodrug for improving oral absorption.

Okaniwa M, Imada T, Ohashi T, Miyazaki T, Arita T, Yabuki M, Sumita A, Tsutsumi S, Higashikawa K, Takagi T, Kawamoto T, Inui Y, Yoshida S, Ishikawa T.

Bioorg Med Chem. 2012 Aug 1;20(15):4680-92. doi: 10.1016/j.bmc.2012.06.015. Epub 2012 Jun 15.

PMID:
22763369
6.

The discovery and initial optimisation of pyrrole-2-carboxamides as inhibitors of p38alpha MAP kinase.

Down K, Bamborough P, Alder C, Campbell A, Christopher JA, Gerelle M, Ludbrook S, Mallett D, Mellor G, Miller DD, Pearson R, Ray K, Solanke Y, Somers D.

Bioorg Med Chem Lett. 2010 Jul 1;20(13):3936-40. doi: 10.1016/j.bmcl.2010.05.011. Epub 2010 May 10.

PMID:
20570148
7.

Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment 13. Synthesis and profiling of a novel amminium prodrug of the HIV-1 attachment inhibitor BMS-585248.

Regueiro-Ren A, Simmermacher-Mayer J, Sinz M, Johnson KA, Huang XS, Jenkins S, Parker D, Rahematpura S, Zheng M, Meanwell NA, Kadow JF.

J Med Chem. 2013 Feb 28;56(4):1670-6. doi: 10.1021/jm301638a. Epub 2013 Feb 12.

PMID:
23374053
8.

Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases.

Liu C, Lin J, Wrobleski ST, Lin S, Hynes J, Wu H, Dyckman AJ, Li T, Wityak J, Gillooly KM, Pitt S, Shen DR, Zhang RF, McIntyre KW, Salter-Cid L, Shuster DJ, Zhang H, Marathe PH, Doweyko AM, Sack JS, Kiefer SE, Kish KF, Newitt JA, McKinnon M, Dodd JH, Barrish JC, Schieven GL, Leftheris K.

J Med Chem. 2010 Sep 23;53(18):6629-39. doi: 10.1021/jm100540x.

PMID:
20804198
9.
10.

The design and synthesis of novel alpha-ketoamide-based p38 MAP kinase inhibitors.

Montalban AG, Boman E, Chang CD, Ceide SC, Dahl R, Dalesandro D, Delaet NG, Erb E, Ernst JT, 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 Mar 15;18(6):1772-7. doi: 10.1016/j.bmcl.2008.02.033. Epub 2008 Feb 16.

PMID:
18325768
11.

Synthesis and SAR of p38alpha MAP kinase inhibitors based on heterobicyclic scaffolds.

Murali Dhar TG, Wrobleski ST, Lin S, Furch JA, Nirschl DS, Fan Y, Todderud G, Pitt S, Doweyko AM, Sack JS, Mathur A, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K.

Bioorg Med Chem Lett. 2007 Sep 15;17(18):5019-24. Epub 2007 Jul 21.

PMID:
17664068
12.

Design, synthesis, and anti-inflammatory properties of orally active 4-(phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38alpha mitogen-activated protein kinase inhibitors.

Hynes J Jr, Dyckman AJ, Lin S, Wrobleski ST, Wu H, Gillooly KM, Kanner SB, Lonial H, Loo D, McIntyre KW, Pitt S, Shen DR, Shuster DJ, Yang X, Zhang R, Behnia K, Zhang H, Marathe PH, Doweyko AM, Tokarski JS, Sack JS, Pokross M, Kiefer SE, Newitt JA, Barrish JC, Dodd J, Schieven GL, Leftheris K.

J Med Chem. 2008 Jan 10;51(1):4-16. Epub 2007 Dec 12.

PMID:
18072718
13.

Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.

Bhide RS, Cai ZW, Zhang YZ, Qian L, Wei D, Barbosa S, Lombardo LJ, Borzilleri RM, Zheng X, Wu LI, Barrish JC, Kim SH, Leavitt K, Mathur A, Leith L, Chao S, Wautlet B, Mortillo S, Jeyaseelan R Sr, Kukral D, Hunt JT, Kamath A, Fura A, Vyas V, Marathe P, D'Arienzo C, Derbin G, Fargnoli J.

J Med Chem. 2006 Apr 6;49(7):2143-6.

PMID:
16570908
14.

Biphenyl amide p38 kinase inhibitors 2: Optimisation and SAR.

Angell RM, Angell TD, Bamborough P, Brown D, Brown M, Buckton JB, Cockerill SG, Edwards CD, Jones KL, Longstaff T, Smee PA, Smith KJ, Somers DO, Walker AL, Willson M.

Bioorg Med Chem Lett. 2008 Jan 1;18(1):324-8. Epub 2007 Oct 17.

PMID:
17981461
15.

Discovery and characterization of non-ATP site inhibitors of the mitogen activated protein (MAP) kinases.

Comess KM, Sun C, Abad-Zapatero C, Goedken ER, Gum RJ, Borhani DW, Argiriadi M, Groebe DR, Jia Y, Clampit JE, Haasch DL, Smith HT, Wang S, Song D, Coen ML, Cloutier TE, Tang H, Cheng X, Quinn C, Liu B, Xin Z, Liu G, Fry EH, Stoll V, Ng TI, Banach D, Marcotte D, Burns DJ, Calderwood DJ, Hajduk PJ.

ACS Chem Biol. 2011 Mar 18;6(3):234-44. doi: 10.1021/cb1002619. Epub 2011 Jan 20.

PMID:
21090814
16.

Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.

Das J, Moquin RV, Pitt S, Zhang R, Shen DR, McIntyre KW, Gillooly K, Doweyko AM, Sack JS, Zhang H, Kiefer SE, Kish K, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K.

Bioorg Med Chem Lett. 2008 Apr 15;18(8):2652-7. doi: 10.1016/j.bmcl.2008.03.019. Epub 2008 Mar 10.

PMID:
18359226
18.

Phosphonooxymethyl prodrugs of the broad spectrum antifungal azole, ravuconazole: synthesis and biological properties.

Ueda Y, Matiskella JD, Golik J, Connolly TP, Hudyma TW, Venkatesh S, Dali M, Kang SH, Barbour N, Tejwani R, Varia S, Knipe J, Zheng M, Mathew M, Mosure K, Clark J, Lamb L, Medin I, Gao Q, Huang S, Chen CP, Bronson JJ.

Bioorg Med Chem Lett. 2003 Nov 3;13(21):3669-72.

PMID:
14552754
19.

Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?

Adkison KK, Barrett DG, Deaton DN, Gampe RT, Hassell AM, Long ST, McFadyen RB, Miller AB, Miller LR, Payne JA, Shewchuk LM, Wells-Knecht KJ, Willard DH Jr, Wright LL.

Bioorg Med Chem Lett. 2006 Feb 15;16(4):978-83. Epub 2005 Nov 15.

PMID:
16290936
20.

Synthesis and evaluation of N-acyl sulfonamides as potential prodrugs of cyclin-dependent kinase inhibitor JNJ-7706621.

Huang S, Connolly PJ, Lin R, Emanuel S, Middleton SA.

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3639-41. Epub 2006 May 6.

PMID:
16682186
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