A5018841510- Synthetic Organic Chemistry Methods
- Asymmetric Synthesis and Catalysis
- Marine Sponges and Natural Products
- Microbial Natural Products and Biosynthesis
- Chemical synthesis and alkaloids
- Chemical Synthesis and Analysis
- Trypanosoma species research and implications
- Synthesis and Biological Evaluation
- Research on Leishmaniasis Studies
- Chemical Synthesis and Reactions
- Carbohydrate Chemistry and Synthesis
- Computational Drug Discovery Methods
- Inorganic and Organometallic Chemistry
- Synthesis and biological activity
- Cancer Treatment and Pharmacology
- Traditional and Medicinal Uses of Annonaceae
- Advanced Synthetic Organic Chemistry
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Rural Development and Agriculture
- Analytical Chemistry and Chromatography
- Asymmetric Hydrogenation and Catalysis
- Organoboron and organosilicon chemistry
- Molecular spectroscopy and chirality
- Enzyme Catalysis and Immobilization
Universidade Estadual de Campinas (UNICAMP)
2016-2025
Universidade Estadual do Centro-Oeste
2021-2024
Universidade Estadual do Paraná
2023
Universidade Federal do Paraná
2015-2021
Pontifícia Universidade Católica de Campinas
2015-2020
Universidade Estadual do Oeste do Paraná
2000-2020
Instituto Federal do Sul de Minas
2018
Universidade Federal de São Carlos
2002-2016
Hospital de Clínicas da Unicamp
2016
Centro Universitário de Desenvolvimento do Centro Oeste
2015
Maspin, a novel serine protease inhibitor (serpin), inhibits tumor invasion and metastasis of mammary carcinoma. We show here that recombinant maspin protein blocks the motility these carcinoma cells in culture over 12 h, as demonstrated by time-lapse video microscopy. Lamellopodia are withdrawn but ruffling continues. Both exogenous expressed transfectants exhibit inhibitory effects on cell shown modified Boyden chamber assays. In addition, three prostatic cancer lines treated with...
Conglobatin is an unusual C2-symmetrical macrodiolide from the bacterium Streptomyces conglobatus with promising antitumor activity. Insights into genes and enzymes that govern both assembly-line production of conglobatin polyketide its dimerization are essential to allow rational alterations be made structure. We have used a rapid, direct in vitro cloning method obtain entire cluster on 41-kbp fragment, encoding modular synthase assembly line. The cloned directs biosynthesis heterologous...
The development of cruzain inhibitors has been driven by the urgent need to develop novel and more effective drugs for treatment Chagas' disease. Herein, we report lead optimization a class noncovalent inhibitors, starting from an inhibitor previously cocrystallized with enzyme (K(i) = 0.8 μM). With goal achieving better understanding structure-activity relationships, have synthesized evaluated series over 40 analogues, leading very promising competitive (8r, IC50 200 nM, K(i) 82 nM)....
The first total synthesis of a spongipyran macrolide, altohyrtin C (spongistatin 2; see picture below), has been realized. spongipyrans derived from marine sponges are among the most potent cytotoxic compounds yet isolated, and exhibit subnanomolar activities against variety human cancer cell lines. While structures proposed for independently isolated altohyrtins spongistatins largely homologous, they differ significantly with regard to internal stereochemical relationships. This discrepancy...
This review summarizes the recent progress which has been made in use of chiral Lewis Acid catalysts Diels-Alder cycloaddition reactions. Chiral containing aluminum, boron, titanium, copper, lanthanides, magnesium and transition-metals are critically reviewed. Structural studies on acid carbonyl complexes synthetic applications systems specifically discussed.
NEW DRUGS.Neglected diseases are a major global cause of illness, long-term disability and death.Chagas' disease is parasitic infection widely distributed throughout Latin America, with devastating consequences in terms human morbidity mortality.The existing drug therapy suffers from combination drawbacks including poor efficacy, resistance serious side effects.In 2009, we celebrate the 100 th anniversary discovery Chagas' disease, facing challenges developing new, safe effective drugs for...
This review covers recent progress in the use of chiral Lewis acid catalysts ene-reactions which involve carbonyl and imine compounds as enophiles. Chiral containing aluminum, titanium, ytterbium copper are critically reviewed. Synthetic applications systems specifically discussed.
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTOne-Pot Preparation of Quinolizidin-2-one and Indolizidin-7-one Ring Systems. Concise Total Syntheses (.+-.)-Myrtine, (.+-.)-Lasubine II, (-)-Indolizidine 223ABRonaldo A. Pilli, Luiz Carlos Dias, Adriano O. MaldanerCite this: J. Org. Chem. 1995, 60, 3, 717–722Publication Date (Print):February 1, 1995Publication History Published online1 May 2002Published inissue 1 February...
A virtual screening conducted with nearly 4 000 compounds from lead-like and fragment-like subsets enabled the identification of a small-molecule inhibitor (1) Trypanosoma cruzi cruzain enzyme, validated drug target for Chagas disease. Subsequent comprehensive structure-based design structure-activity relationship studies led to discovery carbamoyl imidazoles as potent, reversible, competitive inhibitors. The most potent imidazole (45) exhibited high affinity Ki value 20 nM, presenting both...
The total synthesis of (+)-crocacin D is described. convergent asymmetric relies on the use a Stille cross-coupling between an (E)-vinyl stannane with iodide to establish (E,E)-dienamide moiety followed by mild and efficient copper-catalyzed coupling C (Z)-vinyl challenging (Z)-enamide function.
Elaiophylin is an unusual C2 -symmetric antibiotic macrodiolide produced on a bacterial modular polyketide synthase assembly line. To probe the mechanism and selectivity of diolide formation, we sought to reconstitute ring formation in vitro by using non-natural substrate. Incubation recombinant elaiophylin thioesterase/cyclase with synthetic pentaketide analogue presumed monomeric precursor elaiophylin, specifically its N-acetylcysteamine thioester, novel 16-membered macrodiolide. A linear...
Chagas disease causes ~10,000 deaths each year, mainly in Latin America, where it is endemic. The currently available chemotherapeutic agents are ineffective the chronic stage of disease, and lack pharmaceutical innovation for highlights urgent need development new drugs. enzyme cruzain, main cysteine protease Trypanosoma cruzi, has been explored as a validated molecular target drug discovery. Herein, design, modeling studies, synthesis, biological evaluation cyclic imides cruzain inhibitors...
Chagas disease (CD), caused by the flagellate protozoan Trypanosoma cruzi, is a neglected tropical endemic in 21 countries. The only two antiparasitic drugs approved for its treatment, benznidazole and nifurtimox, have significant drawbacks. We present herein optimization of series substituted indoles that were identified through phenotypic screening against T. cruzi. Early lead compounds with balanced potency physicochemical properties advanced to animal studies but showed limited plasma...
A highly convergent and efficient total synthesis of the potent antitumor polyketide (−)-callystatin is described. The required 19 steps from N-propionyl oxazolidinone 23 produced desired product in 3.5% overall yield.
The asymmetric total synthesis of pironetin, a compound that shows plant growth regulatory activity, immunosuppressive as well remarkable antitumoral is described. approach involves the use three very efficient Evans oxazolidinone-mediated syn-aldol condensations, high-yielding coupling between lithium acetylide ethylenediamine complex and tosylate followed by methylation, selective reduction to establish C12−C13 (E) double bond.
The total synthesis of (+)-crocacin C is described. convergent asymmetric relies on the use a regio- and diastereoselective epoxidation an allylic alcohol with m-CPBA followed by epoxide opening Me2CuCNLi2 Stille cross-coupling between E-vinyl stannane 5 iodide 6 to establish (E,E)-dienamide moiety.