A5082796370- Research on Leishmaniasis Studies
- Malaria Research and Control
- Synthesis and biological activity
- Bioactive Natural Diterpenoids Research
- Trypanosoma species research and implications
- Phytochemistry and Bioactive Compounds
- Synthesis and Biological Evaluation
- Quinazolinone synthesis and applications
- Traditional and Medicinal Uses of Annonaceae
- Phytochemistry and Biological Activities
- Mosquito-borne diseases and control
- Essential Oils and Antimicrobial Activity
- Fungal Plant Pathogen Control
- Crystallization and Solubility Studies
- Natural product bioactivities and synthesis
- Insect Pest Control Strategies
- X-ray Diffraction in Crystallography
- Phytochemical compounds biological activities
- Pharmacological Effects of Natural Compounds
- Advanced Breast Cancer Therapies
- Biological Activity of Diterpenoids and Biflavonoids
- Public Health and Environmental Issues
- Drug-Induced Ocular Toxicity
- Inflammasome and immune disorders
- 14-3-3 protein interactions
Central University of Venezuela
2009-2023
Abstract: Tumour relapse, chemotherapy resistance, and metastasis continue to be unsolved issues in cancer therapy. A recent approach has been scrutinise drugs used the clinic for other illnesses modify their structure increase selectivity cells. Chloroquine (CQ) hydroxychloroquine (HCQ), known antimalarials, have successfully treated autoimmune neoplastic diseases. CQ HCQ, well-known lysosomotropic agents, induce apoptosis, downregulate autophagy, tumour microenvironment. Moreover, they...
Twelve 7-chloroquinoline derivatives were designed and synthesized using the principle of molecular hybridization through coupling 2-[2-(7-chloroquinolin-4-ylthio)-4-methylthiazol-5-yl]acetic acid 1 with various benzoyl hydrazines 2a-l. The synthetic compounds tested as antimalarials. Some them showed an efficient in vitro activity inhibitors β-hematin formation vivo a murine model, resulting 8 9 most active ones IC50 values 0.65 ± 0.09 0.64 0.16 µM, respectively. effects on cell viability,...
In the course of searching for bioactive compounds from Croton species Venezuela, two seco-entkaurenes isolated flowers caracasana were evaluated in vitro their effect on cell viability by standard MTT assay nine human cancer lines different origins and one primary culture. Both induced cytotoxicity range 2 to 25 microM caracasine 0.8 12 acid. However, normal fibroblasts lines, HeLa, MCF-7, PC-3, LoVo, X-17, Jurkat E6.1 JCaM1.6, IC50 values acid lower than counterparts. Interestingly, no...
Fisturalines are bromotyrosine compounds isolated from marine sponges. Previous studies have shown antineoplasic, antiviral and antibacterial effects in Vitro; however, the possible of these hematologic malignancies not been assessed.In present study, antiproliferative pro apoptotic Fistularin-3 (F) 11-Deoxyfistularin-3 (DF) were assessed using MTT method annexin V/propidium iodide by flow cytometry cell lines: Jurkat E6.1 U937. In addition, cycle was cytometry.Inhibition proliferative...
A novel series of 2-[2-(7-chloroquinolin-4-ylthio)-4-methylthiazol-5-yl]- N-phenylacetamide derivatives is synthesized via substitution with 2-mercapto-4-methyl-5-thiazoleacetic acid at position 4 4,7-dichloroquinoline to obtain an intermediate acetic derivative. The chemical behavior these reactants was investigated using different reaction conditions optimize the nucleophilic 4. final compounds are prepared a modified version Steglich esterification between 3 and anilines. structures...
Recently, a third subset of Th17 cells has been described. This T helper induces the release chemokines and growth factors causes neutrophil accumulation in several mammalian organs. Pharmacological intervention blocking generation as well IL-17 signaling might prove useful variety diseases including asthma, chronic obstructive pulmonary disease, Crohns cystic fibrosis, multiple sclerosis, psoriatic disease rheumatoid arthritis. Here, we describe patents that address potential...
The coexistence of leishmaniasis, Chagas disease, and neoplasia in endemic areas has been extensively documented. use common drugs the treatment these pathologies invites us to search for new molecules with characteristics. In this research, we report 16 synthetic chalcone derivatives that were investigated leishmanicidal trypanocidal activities as well antiproliferative potential on eight human cancers two nontumor cell lines. final compounds 8−23 obtained using classical base-catalyzed...
A series of heterocyclic chloroquine hybrids, containing a chain two carbon atoms at position four the quinolinic and acting as link between quinoline several benzoyl groups, is synthesized screened in vitro an inhibitor β-hematin formation vivo for its antimalarial activity against chloroquine-sensitive strains Plasmodium berghei ANKA this study. The compounds significantly reduced haeme crystallization, with IC50 values < 10 µM. were comparable to chloroquine's, 1.50 ± 0.01 4c 4e prolonged...
A series of 78 synthetic 7-chloro-(4-thioalkylquinoline) derivatives were investigated for cytotoxic activity against eight human cancer as well 4 non-tumor cell lines. The results showed, with some exceptions, that sulfanyl 5-40 and sulfinyl 41-62 exhibited lower cytotoxicity lines than those well-described sulfonyl N-oxide 63-82. As compound 81, the most pronounced selectivity (compared BJ MRC-5 cells) was observed cells from HCT116 (human colorectal wild-type p53) HCT116p53-/- deleted...
Plants of the Annonaceae family have been used in traditional medicine for treatment a variety ailments including diarrhoea, fever, pain and inflammation. Bioassay-guided separation Xylopia aromatica leaf extract led to isolation two labdane diterpenoids whose structures were identified by 1 H, 13C NMR spectroscopy as 8(17),12E,14-labdatrien-18-oic acid (1) 15,16-dihydroxy-8(17),13(E)-labdadien-19-oic (2), These tested their cytotoxic effect against human HT29 MDA-MB-231, mouse 4T1 cancer...
1D and 2D NMR spectroscopic techniques were used to obtain the complete characterization of cycloart-23-ene-3β-ol (1), isolated from one two species Senefelderopsis belonging Euphorbiaceae family. This is first report, including data, this anti-inflammatory steroid a plant source.