A5102780347- Cancer-related Molecular Pathways
- Cancer therapeutics and mechanisms
- Bioactive Compounds and Antitumor Agents
- Toxin Mechanisms and Immunotoxins
- Synthesis and biological activity
- Eicosanoids and Hypertension Pharmacology
- Microbial Natural Products and Biosynthesis
- Computational Drug Discovery Methods
- Cancer, Hypoxia, and Metabolism
- Marine Sponges and Natural Products
- Essential Oils and Antimicrobial Activity
- Anatomy and Medical Technology
- Biological Activity of Diterpenoids and Biflavonoids
- Click Chemistry and Applications
- Influenza Virus Research Studies
- Morinda citrifolia extract uses
- Mycobacterium research and diagnosis
- Synthesis and pharmacology of benzodiazepine derivatives
- Obstructive Sleep Apnea Research
- Robotic Locomotion and Control
- Cancer, Lipids, and Metabolism
- Virus-based gene therapy research
- Bee Products Chemical Analysis
- Phytochemistry Medicinal Plant Applications
- Cancer Treatment and Pharmacology
Brazilian National Association of Graduate Programs in Communication
2024
Polytechnic Institute of Porto
2024
Rede de Química e Tecnologia
2019-2022
Universidade do Porto
2019-2022
Universidade Lusófona
2018-2020
Technologies pour la Santé
2018
A síndrome da apneia-hipopneia obstrutiva do sono (SAHOS) é caracterizada por obstruções repetidas das vias aéreas superiores, resultando em dessaturação oxiemoglobina e microdespertares. Afeta predominantemente homens sua prevalência aumenta com a idade. Entre os fatores de risco estão tabagismo consumo álcool. etiopatogenia envolve redução ativação dos músculos dilatadores faringe durante o sono, favorecendo colapso aéreas. O diagnóstico feito principalmente meio polissonografia, que...
The Warburg effect is an emerging hallmark of cancer, which has the tumor suppressor p53 as its major regulator. Herein, we unveiled that activation by (S)-tryptophanol-derived oxazoloisoindolinone (SLMP53-1) mediated reprograming glucose metabolism in cancer cells and xenograft human tissue, interfering with angiogenesis migration. Particularly, showed SLMP53-1 regulated glycolysis downregulating transporter 1 (GLUT1), hexokinase-2 (HK2), phosphofructokinase-2 isoform...
Medicinal plants of the Plectranthus genus (Lamiaceae) are known for their ethnopharmacological relevance, mainly against infectious, dermatologic and gastrointestinal pathologies. Three species originated from South Africa, namely P. madagascariensis, neochilus rare porcatus were hereby screened antimicrobial cytotoxic activities related with and/or potential ethnomedicinal uses. Twenty-six extracts prepared by combination extraction methods (infusion, decoction, microwave-assisted,...
Abstract To search for novel p53 activators, four series of ( S )‐ and R )‐tryptophanol‐derived oxazoloisoindolinones were synthesized in a straightforward manner their antiproliferative activity was evaluated the human colorectal cancer HCT116 cell line. Structural optimization hit compound SLMP53‐1 led to identification isoindolinone that found be six‐fold more active, with increased selectivity cells low toxicity normal cells. Binding studies MDM2 showed tryptophanol‐derived...
In silico studies of a library diarylpentanoids led us to the identification potential new MDM2/X ligands. The with best docking scores obeying druglikeness and ADMET prediction properties were subsequently synthesized evaluated for their antiproliferative activity on colon cancer HCT116 fibroblasts HFF-1 cells. effect p53-MDM2/X interactions was through yeast-based assays compounds showing potent in cells low toxicity normal cells, resulting dual inhibitor. Moreover, its significantly...
Hierridin B (6), a methylated hydroquinone isolated from the marine picocyanobacterium Cyanobium sp. LEGE 06113, moderately inhibited growth of colon adenocarcinoma HT-29 cells. Aiming to improve potential antitumor activity this natural product, demethylated analogue, norhierridin (10), as well its structurally-related quinone (9), were synthesized and evaluated for their inhibitory effect on panel human tumor cell lines, including triple-negative breast cancer (TNBC) cells MDA-MB-231,...
New agents are demanded to increase the therapeutic options for osteosarcoma (OS). Although OS is most common bone cancer in children and adolescents, it considered a rare disorder. Therefore, finding adjuvant drugs has potential advance therapy this disease. In study, 3′,4′-dihydroxyflavonol (DiOHF) was investigated assess effects cellular models combination with doxorubicin (Dox). MG-63 U2OS human cells were exposed DiOHF Dox tested cell viability growth. To elucidate inhibitory of DiOHF,...
Natural products are a unique source of lead compounds for medicinal chemistry.Several diterpenes isolated from Plectranthus spp.have been reported to have interesting tuberculostatic activity and P. ornatus Codd.has used in some regions Brazil as an anti-infective.Previously, with halimane labdane skeletons were large quantities Codd.We assessed the anti-mycobacterial these compounds, performing preliminar assay non-virulent strain Mycobacterium smegmatis.The cytotoxicity was tested lactate...
Drug repurposing and rescuing have been widely explored as cost-effective approaches to expand the portfolio of chemotherapeutic agents. Based on reported antitumor properties both trans-cinnamic acids quinacrine, an antimalarial aminoacridine, we antiproliferative two series N-cinnamoyl-aminoacridines recently identified multi-stage antiplasmodial leads. The compounds were evaluated in vitro against three cancer cell lines (MKN-28, Huh-7, HepG2), human primary dermal fibroblasts. One...
TAp73 is a key tumour suppressor protein, regulating the transcription of unique and shared p53 target genes with crucial roles in tumorigenesis therapeutic response. As such, tumours impaired signalling, like neuroblastoma (NBL), activation represents an encouraging strategy, alternative to activation, suppress growth chemoresistance [1]. Actually, NBL one most common childhood solid cancers but despite available treatments, high-risk patients are still characterized by low survival rates,...
The huge impact of cancer is a big concern nowadays. Protein Kinases (PKCs) are attractive anticancer targets due to their involvement in several processes carcinogenesis. Particularly, the isoform δ (PKC-δ) acts as tumor suppressor colon cancer, one most dominant cancers and cause mortality worldwide [1]. Promising bioactive molecules were found Plectranthus genus, mainly diterpene royleanones [1, 2]. 7α-acetoxy-6β-hydroxyroyleanone (Roy) major constituent P. grandidentatus acetonic...
Impairment of the tumour suppressor p53 pathway is a major event in human cancers, making activation one most attractive therapeutic strategies [1]. This work describes synthesis and biological evaluation (R)-tryptophanol-derived bicyclic lactam SYNAP as selective activator with potent anticancer activity against colon cancer [2]. The mechanism action was studied both 2D 3D models adenocarcinoma HCT116 cells wild-type (HCT116 p53+/+) corresponding p53-null isogenic derivative p53-/-), alone...
Cancer is one of the most common causes death worldwide. Many efforts have been made to develop more effective chemotherapeutic drugs. Protein Kinases (PKCs) wide ranging effects in crucial processes tumorigenesis and metastatic dissemination. PKC-δ behaves as tumor suppressor colon cancer, prevalent cancers a leading cause cancer mortality worldwide [1].
With 1.8 million new cases in 2018, colorectal cancer (CRC) is considered one of the most deadliest cancers due to its frequency and high rate mortality. The molecular pathogenesis CRC involves, 40-50 % cases, mutation protein p53. This long-established tumor suppressor inactivated all human cancers, either by protein-protein interaction with main inhibitors MDM2/X or hotspot mutation. Unfortunately, patients mutated p53 gene are likely develop multidrug resistance, which can lead...
Quinones/hydroquinones constitute a family of metabolites, widespread in nature, with wide range biological activities, including cytotoxicity to cancer cells. Recently, hierridin B, methylated hydroquinone derivative C15 aliphatic chain isolated from the marine picocyanobacterium Cyanobium sp. LEGE06,113, was identified as moderate inhibitor growth colon adenocarcinoma HT-29 cell line, GI50 100.2 µM. In order obtain new structurally-related quinone/hydroquinone improved antiproliferative...