Literature DB >> 17570666

Novel tetrahydro-beta-carboline-1-carboxylic acids as inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).

John I Trujillo1, Marvin J Meyers, David R Anderson, Shridhar Hegde, Matthew W Mahoney, William F Vernier, Ingrid P Buchler, Kun K Wu, Syaulan Yang, Syaluan Yang, Susan J Hartmann, David B Reitz.   

Abstract

A structure-activity relationship study was conducted on a series of tetrahydro-beta-carboline-1-carboxylic acid analogs in order to identify the key functionality responsible for activity against the mitogen-activated protein kinase-activated protein kinase 2 enzyme (MK-2). The compounds were further evaluated for their ability to inhibit TNFalpha production in U937 cells and in vivo. These compounds represent a novel structural class of compounds capable of inhibiting MK-2 with remarkable selectivity.

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Year:  2007        PMID: 17570666     DOI: 10.1016/j.bmcl.2007.05.070

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  16 in total

1.  The p38 MAP Kinase Family as Regulators of Proinflammatory Cytokine Production in Degenerative Diseases of the CNS.

Authors:  Adam D Bachstetter; Linda J Van Eldik
Journal:  Aging Dis       Date:  2010-09-24       Impact factor: 6.745

2.  Inhibition of the protein kinase MK-2 protects podocytes from nephrotic syndrome-related injury.

Authors:  Ruma Pengal; Adam J Guess; Shipra Agrawal; Joshua Manley; Richard F Ransom; Robert J Mourey; Rainer Benndorf; William E Smoyer
Journal:  Am J Physiol Renal Physiol       Date:  2011-05-25

3.  Discovery of a Potent Dihydrooxadiazole Series of Non-ATP-Competitive MK2 (MAPKAPK2) Inhibitors.

Authors:  Jun Qin; Pawan Dhondi; Xianhai Huang; Robert Aslanian; James Fossetta; Fang Tian; Daniel Lundell; Anandan Palani
Journal:  ACS Med Chem Lett       Date:  2011-12-23       Impact factor: 4.345

4.  Harmines inhibit cancer cell growth through coordinated activation of apoptosis and inhibition of autophagy.

Authors:  Xinran Geng; Yichang Ren; Fangfang Wang; Danmei Tian; Xinsheng Yao; Youwei Zhang; Jinshan Tang
Journal:  Biochem Biophys Res Commun       Date:  2018-03-01       Impact factor: 3.575

5.  Inhibitory effect of a callophycin A derivative on iNOS expression via inhibition of Akt in lipopolysaccharide-stimulated RAW 264.7 cells.

Authors:  Eun-Jung Park; Li Shen; Dianqing Sun; John M Pezzuto
Journal:  J Nat Prod       Date:  2013-12-03       Impact factor: 4.050

Review 6.  Targeting Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MAPKAPK2, MK2): Medicinal Chemistry Efforts To Lead Small Molecule Inhibitors to Clinical Trials.

Authors:  Mario Fiore; Stefano Forli; Fabrizio Manetti
Journal:  J Med Chem       Date:  2015-11-09       Impact factor: 7.446

7.  Discovery of indolotryptoline antiproliferative agents by homology-guided metagenomic screening.

Authors:  Fang-Yuan Chang; Sean F Brady
Journal:  Proc Natl Acad Sci U S A       Date:  2013-01-09       Impact factor: 11.205

Review 8.  Use of p38 MAPK Inhibitors for the Treatment of Werner Syndrome.

Authors:  Mark C Bagley; Terence Davis; Paola G S Murziani; Caroline S Widdowson; David Kipling
Journal:  Pharmaceuticals (Basel)       Date:  2010-06-04

9.  Enzymatic Strategy for the Resolution of New 1-Hydroxymethyl Tetrahydro-β-carboline Derivatives in Batch and Continuous-Flow Systems.

Authors:  Rita Megyesi; Enikő Forró; Ferenc Fülöp
Journal:  ChemistryOpen       Date:  2016-03-01       Impact factor: 2.911

10.  A computational study on thiourea analogs as potent MK-2 inhibitors.

Authors:  Ming Hao; Hong Ren; Fang Luo; Shuwei Zhang; Jieshan Qiu; Mingjuan Ji; Hongzong Si; Guohui Li
Journal:  Int J Mol Sci       Date:  2012-06-08       Impact factor: 6.208

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