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"Castillo, Juan Carlos"
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America is in the heart
\"Bulosan's semi-autobiographical novel America is in the Heart begins with the narrator's rural childhood in the Philippines and the struggles of land-poor peasant families affected by US imperialism after the Spanish American War of the late 1890s. Carlos's experiences with other Filipino migrant laborers, who endured intense racial abuse in the fields, orchards, towns, cities and canneries of California and the Pacific Northwest in the 1930s, reexamine the ideals of the American dream\"-- Provided by publisher.
Book
Recent Applications of the Multicomponent Synthesis for Bioactive Pyrazole Derivatives
Pyrazole and its derivatives are considered a privileged N-heterocycle with immense therapeutic potential. Over the last few decades, the pot, atom, and step economy (PASE) synthesis of pyrazole derivatives by multicomponent reactions (MCRs) has gained increasing popularity in pharmaceutical and medicinal chemistry. The present review summarizes the recent developments of multicomponent reactions for the synthesis of biologically active molecules containing the pyrazole moiety. Particularly, it covers the articles published from 2015 to date related to antibacterial, anticancer, antifungal, antioxidant, α-glucosidase and α-amylase inhibitory, anti-inflammatory, antimycobacterial, antimalarial, and miscellaneous activities of pyrazole derivatives obtained exclusively via an MCR. The reported analytical and activity data, plausible synthetic mechanisms, and molecular docking simulations are organized in concise tables, schemes, and figures to facilitate comparison and underscore the key points of this review. We hope that this review will be helpful in the quest for developing more biologically active molecules and marketed drugs containing the pyrazole moiety.
Journal Article
Recent Advances in the Synthesis of Organic Thiocyano (SCN) and Selenocyano (SeCN) Compounds, Their Chemical Transformations and Bioactivity
New approaches for the synthesis of organic thio- and selenocyanates, and methods to incorporate them into more complex structures, including a wide variety of heterocyclic and polycylic derivatives, are reviewed. Protocols that convert the SCN and SeCN moieties into the thio and seleno derivatives by transforming the cyano group are also examined. In representative cases, the bioactivity data for these classes of compounds are reviewed.
Journal Article
Synthesis and Biological Studies of Benzobfuran Derivatives: A Review from 2011 to 2022
The importance of the benzo[b]furan motif becomes evident in the remarkable results of numerous biological investigations, establishing its potential as a robust therapeutic option. This review presents an overview of the synthesis of and exhaustive biological studies conducted on benzo[b]furan derivatives from 2011 to 2022, accentuating their exceptional promise as anticancer, antibacterial, and antifungal agents. Initially, the discussion focuses on chemical synthesis, molecular docking simulations, and both in vitro and in vivo studies. Additionally, we provide an analysis of the intricate interplay between structure and activity, thereby facilitating comparisons and profoundly emphasizing the applications of the benzo[b]furan motif within the realms of drug discovery and medicinal chemistry.
Journal Article
N-(3-(tert-Butyl)-1-methyl-1H-pyrazol-5-yl)-4-methyl-N-tosylbenzenesulfonamide
N-(3-(tert-Butyl)-1-methyl-1H-pyrazol-5-yl)-4-methyl-N-tosylbenzenesulfonamide was efficiently synthesized in good yield through a triethylamine-mediated sulfonamidation reaction of 3-(tert-butyl)-1-methyl-1H-pyrazol-5-amine with 4-methylbenzenesulfonyl chloride in acetonitrile at room temperature. The pyrazole-based benzenesulfonamide was fully characterized using FT-IR, NMR, and HMRS techniques.
Journal Article
Cs2CO3‐Promoted Alkylation of 3‐Cyano‐2(1H)‐Pyridones: Anticancer Evaluation and Molecular Docking
Herein, a Cs2CO3‐promoted N‐alkylation of 3‐cyano‐2(1H)‐pyridones containing alkyl groups with diverse alkyl halides to synthesize N‐alkyl‐2‐pyridones over O‐alkylpyridines is reported. The use of alkyl dihalides resulted in complex mixtures of N‐ and O‐alkylated products. The primary factor influencing regioselectivity in these reactions is the electronic effects of substituents on the 2(1H)‐pyridone ring, as evidenced by the preferential formation of O‐alkylpyridines upon the introduction of aryl groups. Remarkably, we efficiently employed CuAAC and Ti(Oi‐Pr)4‐catalyzed amidation reactions to functionalize N‐alkyl‐2‐pyridones containing propargyl and ester groups, leading to the synthesis of 1,2,3‐triazoles and amides, respectively. Moreover, O‐alkylpyridines 10 b and 10 d displayed remarkable selectivity toward the A‐498 renal cancer cell line with growth inhibition percentages (%GI) of 54.75 and 67.64, respectively. The binding modes of compounds 10 b and 10 d to the PIM‐1 kinase enzyme were determined through molecular docking studies. The Cs2CO3‐promoted N‐alkylation of 3‐cyano‐2(1H)‐pyridones with alkyl halides synthesizes N‐alkyl‐2‐pyridones. Functionalization via CuAAC and Ti(Oi‐Pr)4‐catalyzed amidation yields 1,2,3‐triazoles and amides, respectively. O‐alkylpyridines 10b and 10d show selectivity toward A‐498 renal cancer cells. Molecular docking studies reveal their binding to PIM‐1 kinase.
Journal Article
Biochar‐MgO from Soursop Seeds in the Production of Biofuel Additive Intermediates
The conversion of residual biomass from fruit seeds into biochar can be achieved using MgCl2 as an activating agent and calcining at 700 °C. The resulting MgO‐biochars were employed in the aldol condensation reaction between furfural and acetone. This reaction is essential as the first step in the obtention of biofuels derived from biomass. The biochars were characterized through various physicochemical techniques, revealing that the presence of MgO nanoparticles deposited on the carbon surface modifies the structural and acidic‐basic properties of the carbonaceous materials with a graphitic structure. The biochar with a surface content of MgO of 0.34 % w/w enables the achievement of 100 % of selectivity towards 4‐(2‐furanyl)‐3‐buten‐2‐one (I) with quantitative conversions under optimized conditions. This property highlights the potential of using this type of biochar, commonly used for CO2 capture, as a versatile acidic‐basic catalyst, thereby introducing a novel approach to sustainable chemistry. Biochar‐MgO was obtained from residual biomass from soursop seeds and MgCl2 as an activating agent. MgO nanocrystals on the carbon surface that produce lattice defects in graphite structure are responsible of the acid ‐base behavior in aldol condensation between furfural and acetone, to obtain a C8 compounds, which can be used as intermediates in the synthesis of additives of biofuel.
Journal Article
Luteal phase stimulation versus follicular phase stimulation in poor ovarian responders: results of a randomized controlled trial
Background
In young women with poor ovarian response, luteal-phase ovarian stimulation (LPOS) is a potential method for collecting competent oocytes. The aim of this study was to assess the efficacy of LPOS compared with follicular phase ovarian stimulation (FPOS) in young women with poor ovarian response (POR).
Methods
This single-center, prospective, randomized pilot study compared LPOS and FPOS in women with POR fulfilling Bologna criteria who underwent in vitro fertilization at the Instituto Bernabeu. The primary outcome was the number of metaphase II (MII) oocytes obtained by follicular puncture.
Results
Sixty women were included in the study, with 27 women completing LPOS and 30 undergoing FPOS. There was no statistically significant difference in the number of MII oocytes obtained between the LPOS group and the FPOS group (2.1 ± 2.0 vs. 2.6 ± 2.2,
p
= 0.31). Length of stimulation was also similar in both groups (8.35 ± 2.8 vs. 8.15 ± 4.1 days,
p
= 0.69). Similarly, there was no significant difference in the follicle-stimulating hormone total dose, number of cumulus-oocyte complexes, survival rate, fertilization rate, or cancellation rate between groups. A significantly higher Ovarian Sensitivity Index was observed in the LPOS group versus the FPOS group (0.96 vs. 0.57,
p
= 0.037).
Conclusion
LPOS was comparable with FPOS in terms of efficacy and may improve ovarian responsiveness in young women with POR.
Trial registration
ClinicalTrials.gov identifier:
NCT02625532
; EudraCT identifier:
2015–003856-31
.
Journal Article
Synthesis, Spectroscopic, and Thermal Analyses of 2-Oxo-1,2-dihydroquinolin-8-yl 4-chlorobenzoate
The 2-oxo-1,2-dihydroquinolin-8-yl 4-chlorobenzoate was synthesized in good yield using a triethylamine-mediated O-acylation reaction between 8-hydroxyquinolin-2(1H)-one and 4-chlorobenzoyl chloride in acetonitrile at room temperature. This methodology is notable for its clean reaction profile and straightforward procedure. The 2-oxoquinoline derivative was characterized using spectroscopic, spectrometric, and thermal analyses, enabling a comprehensive understanding of its molecular structure and thermal properties.
Journal Article