Literature DB >> 15225717

Synthesis and structure-activity relationships of novel IKK-beta inhibitors. Part 2: Improvement of in vitro activity.

Toshiki Murata1, Mitsuyuki Shimada, Hiroshi Kadono, Sachiko Sakakibara, Takashi Yoshino, Tsutomu Masuda, Makoto Shimazaki, Takuya Shintani, Kinji Fuchikami, Kevin B Bacon, Karl B Ziegelbauer, Timothy B Lowinger.   

Abstract

A series of 2-amino-3-cyano-4-alkyl-6-(2-hydroxyphenyl)pyridine derivatives was synthesized and evaluated as IkappaB kinase beta (IKK-beta) inhibitors. Substitution of an aminoalkyl group for the aromatic group at the 4-position on the core pyridine ring resulted in a marked increase in both kinase enzyme and cellular potencies, and provided potent IKK-beta inhibitors with IC(50) values of below 100 nM.

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Year:  2004        PMID: 15225717     DOI: 10.1016/j.bmcl.2004.05.040

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


  13 in total

1.  Apoptotic effect of genistein on human colon cancer cells via inhibiting the nuclear factor-kappa B (NF-κB) pathway.

Authors:  Yi Luo; Sheng-xiang Wang; Ze-quan Zhou; Zheng Wang; Yan-gao Zhang; Yu Zhang; Peng Zhao
Journal:  Tumour Biol       Date:  2014-08-16

2.  Beyond the frog: the evolution of homology models of human IKKβ.

Authors:  Nicholas Y Palermo; Amarnath Natarajan
Journal:  Bioorg Med Chem Lett       Date:  2011-08-19       Impact factor: 2.823

Review 3.  Inhibitory kappa B Kinases as targets for pharmacological regulation.

Authors:  Carly Gamble; Kathryn McIntosh; Rebecca Scott; Ka Ho Ho; Robin Plevin; Andrew Paul
Journal:  Br J Pharmacol       Date:  2012-02       Impact factor: 8.739

4.  3D QSAR pharmacophore model based on diverse IKKβ inhibitors.

Authors:  Shanthi Nagarajan; Asif Ahmed; Hyunah Choo; Yong Seo Cho; Kwang-Seok Oh; Byung Ho Lee; Kye Jung Shin; Ae Nim Pae
Journal:  J Mol Model       Date:  2010-04-25       Impact factor: 1.810

5.  A selective novel low-molecular-weight inhibitor of IkappaB kinase-beta (IKK-beta) prevents pulmonary inflammation and shows broad anti-inflammatory activity.

Authors:  Karl Ziegelbauer; Florian Gantner; Nicholas W Lukacs; Aaron Berlin; Kinji Fuchikami; Toshiro Niki; Katsuya Sakai; Hisayo Inbe; Keisuke Takeshita; Mina Ishimori; Hiroshi Komura; Toshiki Murata; Timothy Lowinger; Kevin B Bacon
Journal:  Br J Pharmacol       Date:  2005-05       Impact factor: 8.739

6.  An efficient protocol for the synthesis of 2-amino-4,6-diphenylpyridine-3-carbonitrile using ionic liquid ethylammonium nitrate.

Authors:  Swapnil R Sarda; Jagpal D Kale; Sunil K Wasmatkar; Vijay S Kadam; Pravin G Ingole; Wamanrao N Jadhav; Rajendra P Pawar
Journal:  Mol Divers       Date:  2009-03-20       Impact factor: 2.943

7.  Enhanced Tendon-to-Bone Healing via IKKβ Inhibition in a Rat Rotator Cuff Model.

Authors:  Mikhail Golman; Xiaoning Li; Dimitrios Skouteris; Adam A Abraham; Lee Song; Yousef Abu-Amer; Stavros Thomopoulos
Journal:  Am J Sports Med       Date:  2021-01-28       Impact factor: 6.202

8.  IKKβ inhibitor identification: a multi-filter driven novel scaffold.

Authors:  Shanthi Nagarajan; Hyunah Choo; Yong Seo Cho; Kye Jung Shin; Kwang-Seok Oh; Byung Ho Lee; Ae Nim Pae
Journal:  BMC Bioinformatics       Date:  2010-10-15       Impact factor: 3.169

9.  Discovery of a novel IKK-β inhibitor by ligand-based virtual screening techniques.

Authors:  Stefan M Noha; Atanas G Atanasov; Daniela Schuster; Patrick Markt; Nanang Fakhrudin; Elke H Heiss; Olivia Schrammel; Judith M Rollinger; Hermann Stuppner; Verena M Dirsch; Gerhard Wolber
Journal:  Bioorg Med Chem Lett       Date:  2010-10-20       Impact factor: 2.823

10.  Identification of human IKK-2 inhibitors of natural origin (part I): modeling of the IKK-2 kinase domain, virtual screening and activity assays.

Authors:  Esther Sala; Laura Guasch; Justyna Iwaszkiewicz; Miquel Mulero; Maria-Josepa Salvadó; Montserrat Pinent; Vincent Zoete; Aurélien Grosdidier; Santiago Garcia-Vallvé; Olivier Michielin; Gerard Pujadas
Journal:  PLoS One       Date:  2011-02-24       Impact factor: 3.240

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