Biological evaluation of angular disubstituted naphthoimidazoles as anti-inflammatory agents

被引：4

作者：

Cuadrado-Berrocal, Irene ^{[1
]}

Guedes, Gema ^{[2
]}

Estevez-Braun, Ana ^{[2
]}

Hortelano, Sonsoles ^{[3
]}

de las Heras, Beatriz ^{[1
]}

机构：

[1] Univ Complutense Madrid, Fac Farm, Dept Farmacol, Madrid 28040, Spain

[2] Univ La Laguna, Dept Quim Organ, Inst Univ Bioorgan Antonio Gonzalez CIBICAN, E-38206 Tenerife, Spain

[3] Inst Salud Carlos III, IIER, Area Genet Humana, Unidad Terapias Farmacol, Madrid, Spain

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2015年 / 25卷 / 19期

关键词：

Naphthoimidazoles derivatives; Inflammation; Nitric oxide; NF-kappa B; NF-KAPPA-B; INFLAMMATION; CANCER;

D O I：

10.1016/j.bmcl.2015.08.002

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of naphthoimidazoles derivatives (3a-3f) were tested for potential anti-inflammatory activity on lipopolysaccharide (LPS)-treated macrophages. Naphthoimidazole 3e exhibited significant inhibitory effects on nitric oxide (NO) production (IC50 < 10 mu M) and decreased the expression of nitric oxide synthase-2 (NOS-2) and cycloxygenase-2 (COX-2) enzymes. It also inhibited the activation of transcription factor NF-kappa B. Naphthoimidazole 3e might represent a starting point for the synthesis of new anti-inflammatory naphthoimidazoles derivatives. (C) 2015 Elsevier Ltd. All rights reserved.

引用

页码：4210 / 4213

页数：4

共 21 条

[1] NF-κB and the link between inflammation and cancer [J].

DiDonato, Joseph A. ;

Mercurio, Frank ;

Karin, Michael .

IMMUNOLOGICAL REVIEWS, 2012, 246 :379-400

[2] Anti-inflammatory Agents: Present and Future [J].

Dinarello, Charles A. .

CELL, 2010, 140 (06) :935-950

[3] Identification of a pharmacophore for thrombopoietic activity of small, non-peptidyl molecules.: 2.: Rational design of naphtho[1,2-d]imidazole thrombopoietin mimics [J].

Duffy, KJ ;

Price, AT ;

Delorme, E ;

Dillon, SB ;

Duquenne, C ;

Erickson-Miller, C ;

Giampa, L ;

Huang, YF ;

Keenan, RM ;

Lamb, P ;

Liu, NN ;

Miller, SG ;

Rosen, J ;

Shaw, AN ;

Smith, H ;

Wiggall, KJ ;

Zhang, LH ;

Luengo, JI .

JOURNAL OF MEDICINAL CHEMISTRY, 2002, 45 (17) :3576-3578

[4] Missing pieces in the NF-κB puzzle [J].

Ghosh, S ;

Karin, M .

CELL, 2002, 109 :S81-S96

[5] Resolution of inflammation:: Prostaglandin E2 dissociates nuclear trafficking of individual NF-κB Subunits (p65, p50) in stimulated rheumatoid synovial fibroblasts [J].

Gomez, PF ;

Pillinger, MH ;

Attur, M ;

Marjanovic, N ;

Dave, M ;

Park, J ;

Bingham, CO ;

Al-Mussawir, H ;

Abramson, SB .

JOURNAL OF IMMUNOLOGY, 2005, 175 (10) :6924-6930

[6] Monocyte and macrophage heterogeneity [J].

Gordon, S ;

Taylor, PR .

NATURE REVIEWS IMMUNOLOGY, 2005, 5 (12) :953-964

[7]

Guedes G., 2014, THESIS U LA LAGUNA

[8] Unexpected Domino Synthesis of Complex Angular Naphthoimidazoles [J].

Guedes, Gema ;

Lopez-Rodriguez, Matias ;

Ravelo, Angel G. ;

Estevez-Braun, Ana .

EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, 2012, 2012 (29) :5757-5766

[9] The complexity of NF-κB signaling in inflammation and cancer [J].

Hoesel, Bastian ;

Schmid, Johannes A. .

MOLECULAR CANCER, 2013, 12

[10] The IKKNF-κB system:: A treasure trove for drug development [J].

Karin, M ;

Yamamoto, Y ;

Wang, QM .

NATURE REVIEWS DRUG DISCOVERY, 2004, 3 (01) :17-26

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