0000000000349316

AUTHOR

Fernando Albericio

0000-0002-8946-0462

showing 6 related works from this author

Acetic Acid Mediated for One-Pot Synthesis of Novel Pyrazolyl s-Triazine Derivatives for the Targeted Therapy of Triple-Negative Breast Tumor Cells (…

2022

Here, we described the synthesis of novel pyrazole-s-triazine derivatives via an easy one-pot procedure for the reaction of β-dicarbonyl compounds (ethylacetoacetate, 5,5-dimethyl-1,3-cyclohexadione or 1,3-cyclohexadionone) with N,N-dimethylformamide dimethylacetal, followed by addition of 2-hydrazinyl-4,6-disubstituted-s-triazine either in ethanol-acetic acid or neat acetic acid to afford a novel pyrazole and pyrazole-fused cycloalkanone systems. The synthetic protocol proved to be efficient, with a shorter reaction time and high chemical yield with broad substrates. The new pyrazolyl-s-triazine derivatives were tested against the following cell lines: MCF-7 (breast cancer); MDA-MB-231 (tr…

kemiallinen synteesiDMF-DMAlääkekemiabioaktiiviset yhdisteetAnticancer profilePharmaceutical ScienceApoptosisOne-pot synthesisheterosykliset yhdisteetPyrazolyl-s-triazineone-pot synthesis; DMF-DMA; pyrazolyl-<i>s</i>-triazine; anticancer profile; EGFR/PI3K/AKT/mTOR; apoptosisinhibiittoritEGFR/PI3K/AKT/mTOR
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Tiratricol neutralizes bacterial endotoxins and reduces lipopolysaccharide-induced TNF-alpha production in the cell.

2008

Contains fulltext : 70610.pdf (Publisher’s version ) (Closed access) The screening of a commercially available library of compounds has proved a successful strategy for the identification of a lead compound in a drug discovery programme. Here, we analysed 880 off-patent drugs, which initially comprised the Prestwick Chemical library, as sources of bacterial endotoxin neutralizers. We identified 3,3',5-triiodo-thyroacetic acid (tiratricol) as a non-antibacterial compound that neutralizes the toxic lipopolysaccharide.

LipopolysaccharidesendotoxinLipopolysaccharideCelllipopolysaccharide-antagonistsBiology:Enginyeria dels materials [Àrees temàtiques de la UPC]BiochemistryCell LineChemical libraryMicrobiologyLipid ASepsissepsisMiceStructure-Activity Relationshipchemistry.chemical_compoundtumour necrosis factor-alphaDrug DiscoveryEscherichia colimedicineAnimalsDrugs--Designlipid APharmacologyTriiodothyroacetic acidMedicaments -- DissenyTumor Necrosis Factor-alphaDrug discoveryOrganic Chemistrylipopolysaccharidetumour necrosis factor-amedicine.diseaseAnti-Bacterial AgentsEndotoxinsmedicine.anatomical_structurechemistryTriiodothyronineMolecular Medicineseptic shockLead compoundImmunity infection and tissue repair [NCMLS 1]
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Synthesis and Antiproliferative Activity of a New Series of Mono- and Bis(dimethylpyrazolyl)-s-triazine Derivatives Targeting EGFR/PI3K/AKT/mTOR Sign…

2022

Here, we synthesized a newseries of mono- and bis(dimethylpyrazolyl)-s-triazine derivatives. The synthetic methodology involved the reaction of different mono- and dihydrazinyl-s-triazine derivatives with acetylacetone in the presence of triethylamine to produce the corresponding target products in high yield and purity. The antiproliferative activity of the novel mono- and bis(dimethylpyrazolyl)-s-triazine derivatives was studied against three cancer cell lines, namely, MCF-7, HCT-116, and HepG2. N-(4-Bromophenyl)-4-(3,5-dimethyl-1H-pyrazol-1-yl)-6-morpholino-1,3,5-triazin-2-amine 4f, N-(4-chlorophenyl)-4,6-bis(3,5-dimethyl-1H-pyrazol-1-yl)-1,3,5-triazin-2-amine 5c, and 4,6-bis(3,5-dimethy…

General Chemical Engineeringbis(dimethylpyrazolyl)-s-triazine derivativesGeneral Chemistrymono(dimethylpyrazolyl)-s-triazine derivatives
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CCDC 2177427: Experimental Crystal Structure Determination

2022

Related Article: Ihab Shawish, Assem Barakat, Ali Aldalbahi, Walhan Alshaer, Fadwa Daoud, Dana A. Alqudah, Mazhar Al Zoubi, Ma’mon M. Hatmal, Mohamed S. Nafie, Matti Haukka, Anamika Sharma, Beatriz G. de la Torre, Fernando Albericio, Ayman El-Faham|2022|Pharmaceutics|14|1558|doi:10.3390/pharmaceutics14081558

Space GroupCrystallographyCrystal SystemCrystal StructureCell Parameters1-[4-(4-methoxyanilino)-6-(piperidin-1-yl)-135-triazin-2-yl]-1567-tetrahydro-4H-indazol-4-one dimethyl sulfoxide solvateExperimental 3D Coordinates
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CCDC 2163940: Experimental Crystal Structure Determination

2022

Related Article: Ihab Shawish, Assem Barakat, Ali Aldalbahi, Azizah M. Malebari, Mohamed S. Nafie, Adnan A. Bekhit, Amgad Albohy, Alamgir Khan, Zaheer Ul-Haq, Matti Haukka, Beatriz G. de la Torre, Fernando Albericio, Ayman El-Faham|2022|ACS Omega|7|24858|doi:10.1021/acsomega.2c03079

Space GroupCrystallographyCrystal SystemCrystal StructureCell Parameters46-bis(35-dimethyl-1H-pyrazol-1-yl)-N-phenyl-135-triazin-2-amine unknown solvate monohydrateExperimental 3D Coordinates
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CCDC 2163939: Experimental Crystal Structure Determination

2022

Related Article: Ihab Shawish, Assem Barakat, Ali Aldalbahi, Azizah M. Malebari, Mohamed S. Nafie, Adnan A. Bekhit, Amgad Albohy, Alamgir Khan, Zaheer Ul-Haq, Matti Haukka, Beatriz G. de la Torre, Fernando Albericio, Ayman El-Faham|2022|ACS Omega|7|24858|doi:10.1021/acsomega.2c03079

Space GroupCrystallographyCrystal System46-bis(35-dimethyl-1H-pyrazol-1-yl)-N-(4-methoxyphenyl)-135-triazin-2-amine trihydrateCrystal StructureCell ParametersExperimental 3D Coordinates
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