NF-κB-IKKβ pathway as a target for drug development: realities, challenges and perspectives

RHCN Freitas, CAM Fraga - Current drug targets, 2018 - ingentaconnect.com
Background: Nuclear factor ΚB (NF-ΚB) comprises a family of proteins that act as
transcription factors promoting the expression of many genes. Activation of NF-ΚB …

[HTML][HTML] Evaluation of the IKKβ binding of indicaxanthin by induced-fit docking, binding pose metadynamics, and molecular dynamics

M Allegra, M Tutone, L Tesoriere, A Attanzio… - Frontiers in …, 2021 - frontiersin.org
Background: Indicaxanthin, a betaxanthin belonging to the betalain class of compounds, has
been recently demonstrated to exert significant antiproliferative effects inducing apoptosis of …

Discovery of naphthyl‐N‐acylhydrazone p38α MAPK inhibitors with in vivo anti‐inflammatory and anti‐TNF‐α activity

RHCN Freitas, NM Cordeiro… - Chemical biology & …, 2018 - Wiley Online Library
Protein kinases constitute attractive therapeutic targets for development of new prototypes to
treat different chronic diseases. Several available drugs, like tinibs, are tyrosine kinase …

[HTML][HTML] Synthesis and trypanocidal activity of novel pyridinyl-1, 3, 4-thiadiazole derivatives

RHCN Freitas, JMC Barbosa, P Bernardino… - Biomedicine & …, 2020 - Elsevier
Herein, we present the design, synthesis and trypanocidal evaluation of sixteen new 1, 3, 4-
thiadiazole derivatives from N-aminobenzyl or N-arylhydrazone series. All derivatives were …

[HTML][HTML] Discovery of Novel Orally Active Tetrahydro-Naphthyl-N-Acylhydrazones with In Vivo Anti-TNF-α Effect and Remarkable Anti-Inflammatory Properties

NM Cordeiro, RHCN Freitas, CAM Fraga… - PLoS …, 2016 - journals.plos.org
LASSBio-1524 was designed as inhibitor of the IKK-β (kappa β kinase inhibitor) enzyme,
which participates in the activation of the nuclear factor κB (NF-κB) canonical pathway, and …

[HTML][HTML] New 2-amino-pyridinyl-N-acylhydrazones: Synthesis and identification of their mechanism of anti-inflammatory action

N de Morais Cordeiro, RHCN Freitas… - Biomedicine & …, 2020 - Elsevier
Aims The main aim of this paper was the synthesis and the evaluation of the anti-
inflammatory activity of LASSBio-1828 (an amino-pyridinyl-N-acylhydrazone) and its …

Synthesis and pharmacological evaluation of novel isoquinoline N-sulphonylhydrazones designed as ROCK inhibitors

RG Oliveira, FS Guerra, CS Mermelstein… - Journal of Enzyme …, 2018 - Taylor & Francis
In this study, we synthesized a new congener series of N-sulphonylhydrazones designed as
candidate ROCK inhibitors using the molecular hybridization of the clinically approved drug …

Potent immunosuppressive activity of a phosphodiesterase-4 inhibitor N-acylhydrazone in models of lipopolysaccharide-induced shock and delayed-type …

ET Guimarães, TB Dos Santos, DKC Silva… - International …, 2018 - Elsevier
Immunosuppressive drugs are widely used for the treatment of immune-mediated diseases
and inflammation, but the toxicity and side effects of the available immunosuppressors make …

[PDF][PDF] Design, synthesis, biological evaluation, and molecular modeling of inhibitors of enzymes involved in tumor and viral pathologies

G Culletta, M Zappalà, M Tutone, C De Stefano - 2022 - iris.unime.it
Design, synthesis, biological evaluation, and molecular modeling of inhibitors of enzymes
involved in tumor and viral pathologie Page 1 UNIVERSITY OF MESSINA Department of …

[PDF][PDF] NOVO INIBIDOR DE MAPK P38α REDUZ DISFUNÇÃO VENTRICULAR INDUZIDA PELA HIPERTENSÃO ARTERIAL PULMONAR EM RATOS

GF da Silva - 2021 - poscardio.ufrj.br
RESUMO Silva Fernandes Grazielle.“Novo inibidor de MAPK p38α reduz disfunção
ventricular induzida pela hipertensão arterial pulmonar em ratos”. Rio de Janeiro, 2020 …