Literature DB >> 30108896

4-Hydroxy-N-[3,5-bis(trifluoromethyl)phenyl]-1,2,5-thiadiazole-3-carboxamide: a novel inhibitor of the canonical NF-κB cascade.

Agnese C Pippione1, Antonella Federico1, Alex Ducime1, Stefano Sainas1, Donatella Boschi1, Alessandro Barge1, Elisa Lupino2, Marco Piccinini2, Michael Kubbutat3, Jean-Marie Contreras4, Christophe Morice4, Salam Al-Karadaghi5, Marco L Lolli1.   

Abstract

The NF-κB signaling pathway is a validated oncological target. Here, we applied scaffold hopping to IMD-0354, a presumed IKKβ inhibitor, and identified 4-hydroxy-N-[3,5-bis(trifluoromethyl)phenyl]-1,2,5-thiadiazole-3-carboxamide (4) as a nM-inhibitor of the NF-κB pathway. However, both 4 and IMD-0354, being potent inhibitors of the canonical NF-κB pathway, were found to be inactive in human IKKβ enzyme assays.

Entities:  

Year:  2017        PMID： 30108896      PMCID： PMC6084005          DOI： 10.1039/c7md00278e

Source DB:  PubMed          Journal:  Medchemcomm        ISSN： 2040-2503            Impact factor:   3.597


  32 in total

1.  A new IkappaB kinase beta inhibitor prevents human breast cancer progression through negative regulation of cell cycle transition.

Authors:  Akane Tanaka; Susumu Muto; Masayo Konno; Akiko Itai; Hiroshi Matsuda
Journal:  Cancer Res       Date:  2006-01-01       Impact factor: 12.701

Review 2.  Novel NF-κB inhibitors: a patent review (2011 - 2014).

Authors:  Sateesh Kumar Arepalli; Minho Choi; Jae-Kyung Jung; Heesoon Lee
Journal:  Expert Opin Ther Pat       Date:  2015-01-02       Impact factor: 6.674

Review 3.  Non-canonical NF-κB signaling pathway.

Authors:  Shao-Cong Sun
Journal:  Cell Res       Date:  2010-12-21       Impact factor: 25.617

Review 4.  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

5.  Inhibition of NF-{kappa}B improves left ventricular remodeling and cardiac dysfunction after myocardial infarction.

Authors:  Yasuyuki Onai; Jun-Ichi Suzuki; Yasuhiro Maejima; Go Haraguchi; Susumu Muto; Akiko Itai; Mitsuaki Isobe
Journal:  Am J Physiol Heart Circ Physiol       Date:  2006-08-18       Impact factor: 4.733

6.  Design, synthesis, biological evaluation and X-ray structural studies of potent human dihydroorotate dehydrogenase inhibitors based on hydroxylated azole scaffolds.

Authors:  Stefano Sainas; Agnese C Pippione; Marta Giorgis; Elisa Lupino; Parveen Goyal; Cristina Ramondetti; Barbara Buccinnà; Marco Piccinini; Rodolpho C Braga; Carolina H Andrade; Mikael Andersson; Ann-Christin Moritzer; Rosmarie Friemann; Stefano Mensa; Salam Al-Kadaraghi; Donatella Boschi; Marco L Lolli
Journal:  Eur J Med Chem       Date:  2017-02-14       Impact factor: 6.514

7.  A novel IKKbeta inhibitor stimulates adiponectin levels and ameliorates obesity-linked insulin resistance.

Authors:  Junji Kamon; Toshimasa Yamauchi; Susumu Muto; Sato Takekawa; Yusuke Ito; Yusuke Hada; Wataru Ogawa; Akiko Itai; Masato Kasuga; Kazuyuki Tobe; Takashi Kadowaki
Journal:  Biochem Biophys Res Commun       Date:  2004-10-08       Impact factor: 3.575

8.  Inhibition of IkappaB phosphorylation in cardiomyocytes attenuates myocardial ischemia/reperfusion injury.

Authors:  Yasuyuki Onai; Jun-Ichi Suzuki; Tsunekazu Kakuta; Yasuhiro Maejima; Go Haraguchi; Hiroshi Fukasawa; Susumu Muto; Akiko Itai; Mitsuaki Isobe
Journal:  Cardiovasc Res       Date:  2004-07-01       Impact factor: 10.787

9.  IκB kinase-β inhibitor IMD-0354 beneficially suppresses retinal vascular permeability in streptozotocin-induced diabetic mice.

Authors:  Anton Lennikov; Miki Hiraoka; Akira Abe; Shigeaki Ohno; Tomoyuki Fujikawa; Akiko Itai; Hiroshi Ohguro
Journal:  Invest Ophthalmol Vis Sci       Date:  2014-09-09       Impact factor: 4.799

10.  Amelioration of endotoxin-induced uveitis treated with an IκB kinase β inhibitor in rats.

Authors:  Anton Lennikov; Nobuyoshi Kitaichi; Kousuke Noda; Ryo Ando; Zhenyu Dong; Junichi Fukuhara; Satoshi Kinoshita; Kenichi Namba; Miho Mizutani; Tomoyuki Fujikawa; Akiko Itai; Shigeaki Ohno; Susumu Ishida
Journal:  Mol Vis       Date:  2012-10-20       Impact factor: 2.367
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  3 in total

1.  Use of the 4-Hydroxytriazole Moiety as a Bioisosteric Tool in the Development of Ionotropic Glutamate Receptor Ligands.

Authors:  Stefano Sainas; Piero Temperini; Jill C Farnsworth; Feng Yi; Stine Møllerud; Anders A Jensen; Birgitte Nielsen; Alice Passoni; Jette S Kastrup; Kasper B Hansen; Donatella Boschi; Darryl S Pickering; Rasmus P Clausen; Marco L Lolli
Journal:  J Med Chem       Date:  2019-04-18       Impact factor: 7.446

Review 2.  Targeting IKKβ in Cancer: Challenges and Opportunities for the Therapeutic Utilisation of IKKβ Inhibitors.

Authors:  Jack A Prescott; Simon J Cook
Journal:  Cells       Date:  2018-08-23       Impact factor: 6.600

3.  A New NF-κB Inhibitor, MEDS-23, Reduces the Severity of Adverse Post-Ischemic Stroke Outcomes in Rats.

Authors:  Elina Rubin; Agnese C Pippione; Matthew Boyko; Giacomo Einaudi; Stefano Sainas; Massimo Collino; Carlo Cifani; Marco L Lolli; Naim Abu-Freha; Jacob Kaplanski; Donatella Boschi; Abed N Azab
Journal:  Brain Sci       Date:  2021-12-28
  3 in total

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