A5037783757- Synthesis and biological activity
- Bioactive Compounds and Antitumor Agents
- Cancer therapeutics and mechanisms
- Enzyme function and inhibition
- Phenothiazines and Benzothiazines Synthesis and Activities
- Histone Deacetylase Inhibitors Research
- Wnt/β-catenin signaling in development and cancer
- Synthesis and Biological Evaluation
- Immune Cell Function and Interaction
- Cancer Mechanisms and Therapy
- Microtubule and mitosis dynamics
- Cytokine Signaling Pathways and Interactions
- Cholesterol and Lipid Metabolism
- Computational Drug Discovery Methods
- Cancer, Stress, Anesthesia, and Immune Response
- Inflammatory mediators and NSAID effects
- Crystal structures of chemical compounds
- Cellular Mechanics and Interactions
- IL-33, ST2, and ILC Pathways
- Cannabis and Cannabinoid Research
- X-ray Diffraction in Crystallography
- Synthesis and Reactions of Organic Compounds
- Melanoma and MAPK Pathways
- Cancer Treatment and Pharmacology
- Protein Degradation and Inhibitors
Centre Hospitalier Universitaire Sainte-Justine
2025
Université de Montréal
2025
Universidade Federal do Rio de Janeiro
2014-2023
Discovery Air (Canada)
2020
Universidade do Estado do Rio de Janeiro
2017-2018
Abstract Background and Aims Innate immune cells, including dendritic cells (DCs), monocytes (Mono), macrophages (Mac), natural killer (NK), innate lymphoid (ILC), contribute to chronic inflammation in tissues. Here, we characterized the cell landscape inflamed mesenteric lymph nodes (MLNs) of patients with inflammatory bowel diseases (IBD) at single-cell level. Methods Surgically resected colonic MLNs were obtained from Crohn’s disease (CD; n = 3), ulcerative colitis (UC; non-inflamed UC (n...
Abstract Targeting histone deacetylases (HDACs) and phosphatidylinositol 3‐kinases (PI3Ks) is a very promising approach for cancer treatment. This manuscript describes the design, synthesis, in vitro pharmacological profile, molecular modeling of novel class N ‐acylhydrazone (NAH) derivatives that act as HDAC6/8 PI3Kα dual inhibitors. The surprising selectivity may be related to differences conformation active site. Cellular studies showed these compounds HDAC6 inhibition PI3/K/AKT/mTOR...
Tumor aggressiveness is usually associated with metastasis. MDA-MB 231, a triple-negative breast cancer (TNBC), an aggressive type of and early The Rho/ROCK pathway key regulator cell motility involving cytoskeleton regulation through stabilization actin filaments stress fiber formation. In this study we show that Fasudil, ROCK inhibitor, inhibited the migration 231 A549 cells, without altering viability these cells at concentration 10 μM, modified tumor morphology, disorganization fibers...
Migration and invasion are hallmarks of cancer cells that allow their dissemination to other tissues. Studying the cellular molecular basis cell migration can help us understand control metastasis. Many membrane molecules have been described as being involved in tumor migration, among them is cholesterol. In present study we investigated role cholesterol breast cells. The human mammary gland/breast epithelial line MDA-MB 231 was used depleted with methyl-β-cyclodextrin (MbCD). Cell measured...
Background: Prostate cancer is the second most frequently diagnosed malignancy worldwide. Here, cytotoxic and antimetastatic effects of a new HDAC6/8 inhibitor, LASSBio-1911, dual-PI3K/HDAC6 LASSBio-2208, were evaluated against PC3 prostate cell line. Methods: A MTT assay was used to assess viability. Annexin V/propidium iodide (PI) detect apoptotic death analyze cycle distribution. Interleukin 6 (IL-6) levels measured by ELISA. scratch performed migration, expression proteins estimated...
In this study, we synthesized a new congener series of N-sulphonylhydrazones designed as candidate ROCK inhibitors using the molecular hybridization clinically approved drug fasudil (1) and IKK-β inhibitor LASSBio-1524 (2). Among compounds, N-methylated derivative 11 (LASSBio-2065) showed best inhibitory profile for both isoforms, with IC50 values 3.1 3.8 µM ROCK1 ROCK2, respectively. Moreover, these compounds were also active in scratch assay performed human breast cancer MDA-MB 231 cells...
Novel isatinspirooxazine derivatives were designed and synthesized as potential anti-proliferative agents.The new compounds obtained from aldol condensation reactions between isatin 3-(hydroxyimino)butan-2-one in the presence of an organic base order to generate adduct, followed by cyclization trifluoroacetic acid, providing desired isatinspirooxazines 30 80% yield.All compounds, including starting material synthetic intermediates, tested for vitro activity against cell lines MCF-7 MDA-MB231...
In this work, we report the synthesis of three series carbohydrate-based benzo[f]indole-4,9-diones and amino-1,4-naphthoquinone derivatives evaluated their cytotoxic activity against eight human cancer cell lines.Several compounds showed a promising toward tumor lines (half maximal inhibitory concentration (IC 50 ) < 10.0 μM).The importance substitution pattern quinone on antitumor was also discussed.3-Carboethoxy-2-methyl-benzo[f]indole-4,9-dione were more than parent...
Metastatic melanoma patients have a poor prognosis with responsiveness to chemotherapy. BRAF V600E mutations been detected in ~40% of patients. Vemurafenib is an oral agent licensed for mutation-positive inoperable and metastatic melanoma, which already presents resistance that leads patient relapse the serious side effects. In our study, we synthesized 5 new vemurafenib analogs, RF-86A, RF-87A, RF-94A, RF-94B RF-96B, structural improve-ments, order increase anti-proliferative...
Triple-negative breast cancer (TNBC) is a subtype of with poor clinical outcome, and currently no effective targeted therapies are available. Indole compounds have been shown to potential antitumor activity against various cells. In the present study, we found that new four benzo[
The ability of cancer cells to undergo invasion and migration is a prerequisite for tumor metastasis. Rho, Ras-related small GTPase, the Rho-associated coiled coil–containing protein kinases (Rho kinases, ROCK1 ROCK2), are key regulators focal adhesion, actomyosin contraction, thus cell motility. concept Rho Kinase inhibition as an antimetastatic therapy can now be clinically explored. Therefore, it great interest investigate whether Fasudil kinase inhibitor) affects early events in human...
Many patients with metastatic tumors have substantially worse survival in comparison those nonmetastatic tumors. The ability of cancer cells to undergo invasion and migration is a prerequisite for tumor metastasis these events became targets the development new antimetastatic drugs. Rho kinases, ROCK1 ROCK2, are key regulators focal adhesion, actomyosin contraction, thus cell motility. In this regard our group synthesized two sulfonylhydrazones, analogous Fasudil (a classic kinase...