• Publications
  • Influence
LASSBio-1135: A Dual TRPV1 Antagonist and Anti-TNF-Alpha Compound Orally Effective in Models of Inflammatory and Neuropathic Pain
LASSBio-1135, besides being a weak COX-2 inhibitor, is a non-competitive TRPV1 antagonist and a TNF-α inhibitor and as a multitarget compound is orally efficacious in a model of neuropathic pain without presenting hyperthermia. Expand
N-Acylhydrazones as drugs.
This review highlights the detailed comprehensive assessment and therapeutic landscape of bioactive NAH motif scaffolds in preclinical and clinical studies published to date and their promise and associated challenges in current and future drug discovery of NAH-based drugs that will progress to clinical use. Expand
Filtering promiscuous compounds in early drug discovery: is it a good idea?
The so-called pan assay interference compounds (PAINS) or promiscuous compounds could be in fact assay artifacts, false positives or, simply, bright chemical matter (BCM) composed of privileged scaffolds, as it is proposed here. Expand
Drug hybridization strategies: before or after lead identification?
  • C. A. Fraga
  • Biology, Medicine
  • Expert opinion on drug discovery
  • 21 May 2009
Possible ways of exploring molecular hybridization strategies to plan new effective dual or symbiotic drug candidates are described. Expand
Duvelisib: A 2018 Novel FDA-Approved Small Molecule Inhibiting Phosphoinositide 3-Kinases
This review provides a series of information about duvelisib, such as the development of clinical trials for LLC/SLL and FL and the steps used for its synthesis. Expand
ROCK inhibition with Fasudil induces beta-catenin nuclear translocation and inhibits cell migration of MDA-MB 231 human breast cancer cells
Fasel, a ROCK inhibitor, inhibited the migration of MDA-MB 231 and A549 cells, without altering the viability of these cells at the concentration of 10 μM, modified tumor cell morphology, with disorganization of stress fibers and promotes activation of the canonical-Wnt/beta-catenin pathway. Expand
Beyond the Selective Inhibition of Histone Deacetylase 6.
The structure-activity and structureselectivity relationships of HDAC6 inhibitors were described, which were divided into two main classes, bulky and lipophilic cap groups and inhibitors with phenyl linkers. Expand
Structural basis for the agonist action at free fatty acid receptor 1 (FFA1R or GPR40)
A review of the structure–activity relationships of GPR40 agonists with a focus on the main strategies of medicinal chemistry used to develop each one of the main structural patterns exploited for this receptor. Expand
Design, Synthesis, and Pharmacological Evaluation of First‐in‐Class Multitarget N‐Acylhydrazone Derivatives as Selective HDAC6/8 and PI3Kα Inhibitors
The design, synthesis, in-vitro pharmacological profile, and molecular modeling of a novel class of N‐acylhydrazone (NAH) derivatives that act as HDAC6/8 and PI3Kα dual inhibitors are described. Expand
Discovery of Novel Orally Active Tetrahydro-Naphthyl-N-Acylhydrazones with In Vivo Anti-TNF-α Effect and Remarkable Anti-Inflammatory Properties
The data indicate that the tested compounds have anti-inflammatory activity, which may be related to inhibition of leukocyte migration, reducing the production of NO, TNF-α and ROS. Expand