A5044415892- Synthesis and biological activity
- Plant-derived Lignans Synthesis and Bioactivity
- Click Chemistry and Applications
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Synthetic Organic Chemistry Methods
- Synthesis of Organic Compounds
- Metal complexes synthesis and properties
- Traditional and Medicinal Uses of Annonaceae
- Quinazolinone synthesis and applications
- Computational Drug Discovery Methods
- Asymmetric Synthesis and Catalysis
- Cancer therapeutics and mechanisms
- Magnolia and Illicium research
- Synthesis and Biological Evaluation
- Carbohydrate Chemistry and Synthesis
- Bioactive Compounds and Antitumor Agents
- Biological Activity of Diterpenoids and Biflavonoids
- Synthesis and Characterization of Heterocyclic Compounds
- Synthesis and Reactions of Organic Compounds
- Parasites and Host Interactions
- Chemical Synthesis and Analysis
- Cyclopropane Reaction Mechanisms
- Microbial Natural Products and Biosynthesis
- DNA and Nucleic Acid Chemistry
Instituto de Investigación Biomédica de Salamanca
2015-2025
Universidad de Salamanca
2016-2025
Centro de Investigación del Cáncer
2004-2005
California Institute of Technology
1997-2000
University of California, Berkeley
1997-2000
Introduction Schistosomiasis, one of the current Neglected Tropical Diseases (NTDs) affects over 230 million people globally, with nearly 700 at risk in more than 74 countries. Praziquantel (PZQ) has served as primary treatment for past four decades; however, its effectiveness is limited it solely eliminates adult worms. In regions where infections are frequent, PZQ exhibits only temporary efficacy and restricted potential to disrupt prolonged transmission disease.
By synthesis and biological studies of new naphthalene analogues combretastatins, we have found that the is a good surrogate for isovanillin moiety (3-hydroxy-4-methoxyphenyl) combretastatin A-4, always generating highly cytotoxic when combined with 3,4,5-trimethoxyphenyl or related systems. On other hand, replaces moiety, activity largely decreased. The most which also produce inhibition tubulin polymerization, exerted their antimitotic effects through microtubule network disruption...
Colchicine site ligands with indole B rings are potent tubulin polymerization inhibitors. Structural modifications at the 3-position of 1-methyl-5-indolyl-based isocombretastatins (1,1-diarylethenes) and phenstatins endowed them anchors for further derivatization resulted in highly compounds. The substituted derivatives displayed cytotoxicity against several human cancer cell lines due to inhibition, as shown by cycle analysis, confocal microscopy, inhibitory activity studies promoted...
Polyamides containing N-methylimidazole (Im) and N-methylpyrrole (Py) amino acids can be combined in antiparallel side-by-side dimeric complexes for sequence-specific recognition the minor groove of DNA. Covalently linking polyamide subunits has led to designed ligands with both increased affinity specificity. Simple aliphatic acid linkers serve as internal guide residues turn vs extended binding a head-to-tail-linked motif. sequence composition ImPyPy-X-PyPyPy incremental length (X =...
The design of colchicine site ligands on tubulin has proven to be a successful strategy develop potent antiproliferative drugs against cancer cells. However, the structural requirements binding endow with low aqueous solubility. In this work, benzothiazole scaffold is used design, synthesize, and evaluate new family exhibiting high water compounds exerted activity several human cell lines, due polymerization inhibition, showing selectivity toward cells in comparison non-tumoral HEK-293...
Tubulin is a well-validated target for herbicides, fungicides, anti-parasitic, and anti-tumor drugs. Many of the non-cancer tubulin drugs bind to its colchicine site but no colchicine-site anticancer drug available. The composed three interconnected sub-pockets that fit their ligands modify others' preference, making design molecular hybrids (that more than one sub-pocket) difficult task. Taking advantage eighty published X-ray structures in complex with bound site, we generated an ensemble...
Urea receptor 1 based on two (1-amino-8-amido-3,6-dichloro)carbazole units shows a strong association with dicarboxylate anions such as oxalate, malonate and succinate guests through multiple hydrogen bonds from the carbazole, urea amide NH groups. (1)H NMR complexation studies exhibit high values of constants in DMSO-d(6). X-ray structures : complexes oxalate their ditetrabutylammonium salts were obtained. A modelling study complex (as its diTBA salt) showed more reduced geometric...
An asymmetric concise total synthesis of the (+)-seco-C-oleanane 1 was accomplished. The successful route to this natural product involves as key step a stepwise regio- and stereocontrolled catalytic radical polyene cascade cyclization from preoleanatetraene oxide (16), process mediated by Cp(2)TiCl. use single-electron-transfer complex permits mild conditions without using unnecessary prefunctionalizations stops at bicyclic level. Theoretical data revealed high activation energy for third...
IMP dehydrogenase (IMPDH) is an essential enzyme that catalyzes the rate-limiting step in de novo guanine nucleotide biosynthetic pathway. Because of its involvement control cell division and proliferation, IMPDH represents a therapeutic for managing several diseases, including microbial infections cancer. must be tightly regulated, but molecular mechanisms responsible physiological regulation remain unknown. To this end, we recently reported important role adenine mononucleotides bind to...