Juan José Vaquero

Juan José Vaquero López
Group coordinator
Full Professor

Publons: E-8310-2012

• Emeritus Professor, Universidad de Alcalá (2023)
• Full Professor Organic Chemistry, Universidad de Alcalá (1998)
• Associate Professor, Universidad de Alcalá (1986)
• Interim Associate Professor, Universidad de Alcalá (1982-1986)
• Postdoctoral researcher, Prof. Charles Rees group, Imperial College London (1985-1986)
• FPI grant (Ministerio de Educación y Ciencia) Universidad de Alcalá (1978-1981)
• Graduated at the Universidad Complutense de Madrid (1976)

Coordinator of Biological Chemistry group, created in 1995, with chemists, pharmacists and molecular biologists developing projects in the field of Medical, Heterocyclic and Bioorganics Chemistry. During this time, the research has been carried out in different lines, among which the following stand out due to their duration and results: Chemistry and applications of heteroaromatic cations in cell staining and bioimaging, synthesis of heterocycles and bioactive alkaloids, design and synthesis of bioactive compounds against targets involved in renal and chemical disease, and applications of azaborines.
In this period, we have participated in 27 R&D&I projects financed in competitive calls from public administrations (Plan Nacional, Comunidad Autónoma de Madrid, Instituto de Salud Carlos III (RETICS), INNPACTO), having acted as PI in 18 of these projects. It has participated in 59 non-competitive R&D&I contracts, agreements or projects financed with administrations and public entities and private companies, acting as PI in 43 of these contracts/projects. The results obtained are summarized in 175 publications in JCR-indexed journals, 29 patents (2 international, 4 PCT), 220 contributions to national and international conferences and the supervision of 24 Doctoral Theses, 10 Theses and 8 Master’s Theses.
He has participated as co-author in three book chapters published by international publishers (Jai Press LTD, UK and Wiley-VCH Verlag) and co-editor together with Prof. Jose Barluenga and Prof. Julio Alvarez-Builla of the 4 volumes of Modern Heterocyclic Chemistry. pp. 1 – 2445 (Germany), WILEY-VCH Verlag GmbH & Co. KGaA (2011).
He has held the academic positions of Dean of the Faculty of Chemistry of the Universidad de Alcalá (2000-2006), Vice-Dean of the Faculty of Science (1987-2000), Scientific Director of the Centre for Applied Chemistry and Biotechnology of the University of Alcalá (2009-2011), 2012-2014, 2015-2017, 2018…), Coordinator by the Universidad de Alcalá of the Inter-University Master in Drug Discovery (2013…) and Trustee appointed by the Universidad de Alcalá in the Board of Trustees of the IMDEA-AGUA Institute of the Comunidad de Madrid (2009…). He has also chaired the Madrid Territorial Section of the Spanish Royal Society of Chemistry for the period 2006-2011.

Publications in the group

Synthesis of Seven- and Eight-Membered Rings by a Brønsted Acid Catalyzed Cationic Carbocyclization of Biphenyl Embedded Enynes.
Org Lett. 2024 Apr 26;26(16):3343-3348. doi: 10.1021/acs.orglett.4c00647. Epub 2024 Apr 11.
Plaza 3055
Advanced Synthesis & Catalysis. 2024; 366(2):232 -240.
1,2,3-Benzotriazine Synthesis by Heterocyclization of p-Tosylmethyl Isocyanide Derivatives.
J. Org. Chem. 2023, 88, 14131
One-Pot (3 + 2) Cycloaddition-Isomerization-Oxidation of 2,2,2-Trifluorodiazoethane and Styryl Derivatives.
J Org Chem. 2023, 88, 11258
β-Functionalization of 4 a-aza-8 a-boranaphthalene via Iridium-catalyzed C−H Borylation.
Adv. Synth. Catal. 2023, 365, 2545
Visible-Light-Mediated Regioselective Chlorosulfonylation of Acrylamides.
Synthesis 2023, 55, 1783
Gold-catalyzed endo-selective cyclization of alkynylcyclobutanecarboxamides: synthesis of cyclobutane-fused dihydropyridones.
Org Biomol Chem. 2023, 21, 2705
Synthesis of Five-Membered Organoborate Heterocycles via a Metal-Free Carboboration and Their Use in Cross-Coupling Reactions.
Synthesis 2023, 55, 1260
Synthesis of Phenanthrene-Based Polycycles by Gold(I)-Catalyzed Cyclization of Biphenyl-Embedded Trienynes.
Adv. Synth. Catal. 2022, 364, 3960
Highly efficient unbridged D-A+(D) chromophores based on the quinolizinium cation for nonlinear optical (NLO) applications.
Dyes Pigm. 2022, 205, 110323.
Synthesis of BN-Polyarenes by a Mild Borylative Cyclization Cascade.
Org Lett. 2022, 24, 5860
Steviol glycosides as an alternative osmotic agent for peritoneal dialysis fluid.
Front Pharmacol. 2022, 13, 868374
Insight into the mechanism of molecular recognition between human Integrin-Linked Kinase and Cpd22 and its implication at atomic level.
J Comput Aided Mol Des. 2022 Aug;36(8):575-589. doi: 10.1007/s10822-022-00466-1.
Metal-Free Temperature-Controlled Regiodivergent Borylative Cyclizations of Enynes: BCl(3) -Promoted Skeletal Rearrangement.
Angew Chem Int Ed Engl. 2022, e202205651
Pyridazino-pyrrolo-quinoxalinium salts as highly potent and selective leishmanicidal agents targeting trypanothione reductase.
Eur J Med Chem. 2022, 227, 113915
1,10a-Dihydro-1-aza-10a-boraphenanthrene and 6a,7-Dihydro-7-aza-6a-boratetraphene: Two New Fluorescent BN-PAHs.
J Org Chem. 2021 Nov 22. doi: 10.1021/acs.joc.1c01095.
Two-photon activated precision molecular photosensitizer targeting mitochondria.
2021; 4(1):142.
A Computer-Driven Scaffold-Hopping Approach Generating New PTP1B Inhibitors from the Pyrrolo%1,2-a%quinoxaline Core.
ChemMedChem. 2021 Sep 16;16(18):2895-2906. doi: 10.1002/cmdc.202100338.
Enantioselective Copper-Catalyzed Synthesis of Trifluoromethyl-Cyclopropylboronates.
Org Lett. 2021 Aug 6;23(15):6174-6178. doi: 10.1021/acs.orglett.1c02420.
Pyrrolo%1,2-a%quinoxal-5-inium salts and 4,5-dihydropyrrolo%1,2-a%quinoxalines: Synthesis, activity and computational docking for protein tyrosine phosphatase 1B.
Bioorg Med Chem. 2021 Jul 3; 44:116295.
Tripeptides as Integrin-Linked Kinase Modulating Agents Based on a Protein-Protein Interaction with α-Parvin.
ACS Med Chem Lett. 2021 Jul 15;12(11):1656-1662. doi: 10.1021/acsmedchemlett.1c00183.
Recent developments in the chemistry of BN-aromatic hydrocarbons.
Adv. Heterocycl. Chem. 2021 Mar 28; :197-259.
A new family of fluorescent pyridazinobenzimidazolium cations with DNA binding properties.
Dyes and Pigments. 2021 Aug 1; :109443.
Selective Synthesis of Phenanthrenes and Dihydrophenanthrenes via Gold-Catalyzed Cycloisomerization of Biphenyl Embedded Trienynes.
Org Lett. 2020, 22, 8464
Gold-Catalyzed Synthetic Strategies towards Four-Carbon Ring Systems.
Catalysts 2020, 22, 1178
Pyrrolo%@5B1,2-a%@5Dquinoxalines: Insulin Mimetics that Exhibit Potent and Selective Inhibition against Protein Tyrosine Phosphatase 1B.
ChemMedChem 2020, 15, 1788
The pHLIP system as a vehicle for microRNAs in the kidney.
Nefrologia. 2020, 40, 491
Practical Solvent-Free Microwave-Assisted Hydroboration of Alkynes.
Eur. J. Org. Chem. 2020, 3024
Expanding the BN-embedded PAH family: 4a-aza-12a-borachrysene.
Chem Commun 2020, 56, 3669
Synthesis and Photophysical Behavior of a Highly Fluorescent Family of Unsymmetrical Organoboron Complexes Containing 5-(Pyridin-2-ylmethylene)imidazolidine-2,4-dione Moieties.
J Org Chem. 2020, 85, 441
A New Member of the BN-Phenanthrene Family: Understanding the Role of the B-N Bond Position.
J Org Chem. 2019, 84, 7113
Remarkable effect of alkynyl substituents on the fluorescence properties of a BN-phenanthrene.
Beilstein J. Org. Chem. 2019, 15, 1257
NIK as a Druggable Mediator of Tissue Injury.
Trends Mol Med. 2019, 25, 341
Synthesis, Functionalization, and Optical Properties of 1,2-Dihydro-1-aza-2-boraphenanthrene and Several Highly Fluorescent Derivatives.
Org Lett. 2019, 21, 2550
Regiodivergent Electrophilic Cyclizations of Alkynylcyclobutanes for the Synthesis of Cyclobutane-Fused O-Heterocycles.
J. Org. Chem. 2019, 84, 9, 5712
MAP3K kinases and kidney injury.
Nefrologia 2019, 39, 568
Discovery of potent calpain inhibitors based on the azolo-imidazolidenone.
Eur J Med Chem. 2018, 157, 946
C-H Functionalization of BN-Aromatics Promoted by Addition of Organolithium Compounds to the Boron Atom.
Org Lett. 2018, 20, 4902
gamma-Carboline Synthesis by Heterocyclization of TosMIC Derivatives.
J Org Chem. 2018, 83, 6623
A Tricin Derivative from Deschampsia antarctica Desv. Inhibits Colorectal Carcinoma Growth and Liver Metastasis through the Induction of a Specific Immune Response.
Mol Cancer Ther. 2018 May;17(5):966-976. doi: 10.1158/1535-7163.MCT-17-0193. Epub 2018 Feb 26.
Dibenzopyridoimidazocinnolinium cations: a new family of light-up fluorescent DNA probes.
Org. Chem. Front. 2018, 5, 1916
Synthesis of functionalized helical BN-benzo%c%phenanthrenes.
Chem Commun 2018, 54, 2467
Azonia aromatic heterocycles as a new acceptor unit in D-π-A%@2B vs D-A%@2B nonlinear optical chromophores.
Dyes Pigm. 2017, 144, 17
Microwave-assisted pyrolysis of Mediterranean forest biomass waste: Bioproduct characterization.
J Anal Appl Pyrolysis 2017, 127, 278
Synthesis, Optical Properties, and Regioselective Functionalization of 4a-Aza-10a-boraphenanthrene.
Org Lett. 2017, 19, 3458
Imidazopyridinium cations: A new family of azonia aromatic heterocycles with applications as DNA intercalators.
Dyes Pigm. 2017, 138, 135
Quinolizinium as a new fluorescent lysosomotropic probe.
Biorg. Med. Chem. Lett. 2017, 27, 203
Halogen-containing thiazole orange analogues - new fluorogenic DNA stains.
Beilstein J. Org. Chem. 2017, 13, 2902
Recent Advances in the Synthesis of Azonia Aromatic Heterocycles.
J Org Chem. 2016, 81, 10126
Synthesis of 1-Substituted Isoquinolines by Heterocyclization of TosMIC Derivatives: Total Synthesis of Cassiarin A.
Org Lett. 2016, 18, 3378
Highly Fluorescent Green Fluorescent Protein Chromophore Analogues Made by Decorating the Imidazolone Ring.
Chem. Eur. J. 2015, 21, 18758
Assembly of New Merocyanine Chromophores with a 1,8-Naphthalimide Core by a New Method for the Synthesis of the Methine Function.
Aust. J. Chem. 2015, 68, 1399
Nonlinear Emission of Quinolizinium Based Dyes With Application in Fluorescence Lifetime Imaging.
J. Phys. Chem. A 2015, 119, 11, 2351
Azonia Aromatic Cations by Ring-Closing Metathesis: Synthesis ofAzaquinolizinium Cations.
Eur J Org Chem. 2015, 6, 4214
Synthesis and biological evaluation of pyridazino%@5B1′,6′:1,2%@5Dpyrido%@5B3,4-b%@5Dindolinium and pyridazino%@5B1,6-a%@5Dbenzimidazolium salts as anti-inflammatory agents.
Eur. J. Med. Chem. 2015, 93, 83
Isoquinoline synthesis by heterocyclization of tosylmethyl isocyanide derivatives: total synthesis of mansouramycin B.
Org Lett. 2015, 17, 78
Targeting DNA with small molecules: a comparative study of a library of azonia aromatic chromophores.
Org Biomol Chem. 2015, 13, 527
Efficient synthesis of an indoloquinolizinium alkaloid selective DNA-binder by ring-closing metathesis.
Org Lett. 2014, 16, 3464
Microwave-assisted synthesis of potent PDE7 inhibitors containing a thienopyrimidin-4-amine scaffold.
Org Biomol Chem. 2014, 12, 4233
Cucurbit%n%urils as a potential fine-tuned instrument for modifying photophysical properties of D–π–A+–π–D “push–pull” chromophores.
Dyes Pigm. 2014, 103, 106
Novel charged NLO chromophores based on quinolizinium acceptor units.
Dyes Pigm. 2014, 101, 116
Remote aryl cyanation via isocyanide-cyanide rearrangement on tosylmethyl isocyanide derivatives.
Org Lett. 2013 Jul 5;15(13):3388-91. doi: 10.1021/ol401433x. Epub 2013 Jun 24.
A cascade reaction of azolopyrimidines. Synthesis of unusual indole and azaindole derivatives.
Chem. Commun. 2012, 48, 9171
Superior Neuroprotective Efficacy of LAU-0901, a Novel Platelet-Activating Factor Antagonist, in Experimental Stroke.
Translational Stroke Research 2012, 3, 154
Synthesis of 9,9′-%1,2-Ethanediylbis(oxymethylene)%bis-2-amino-1,9-dihydro-6H-purin-6-one, an Impurity of Acyclovir.
Molecules 2012, 17, 8735
New losartan-hydrocaffeic acid hybrids as antihypertensive-antioxidant dual drugs: Ester, amide and amine linkers
Eur. J. Med. Chem 2012, 50, 90
Radical Intramolecular Arylation of Pyridinium Salts: A Straightforward Entry to 7-Hydroxypyrido%2,1‐a%isoquinolinylium Salts /
Eur. J. Org. Chem. 2011, 619
An environmentally benign procedure for the synthesis of substituted 2-thiobenzothiazoles, 2-thiobenzoxazoles, 2-thiobenzimidazoles, and 1,3-oxazolopyridine-2-thiols.
Monatsh. Chem. 2011, 142, 895
Synthesis of novel tetracationic asymmetric monomeric monomethine cyanine dyes – highly fluorescent dsDNA probes /
Coloration Technology. 2011, 127, 69
Environmental Risk Assessment of Emerging Pollutants in Water: Approaches Under Horizontal and Vertical EU Legislation /
Critical Reviews in Environmental Science and Technology 2011, 41, 699
Ring-Closing Metathesis Approach to Heteroaromatic Cations: Synthesis of Benzo%a%Dquinolizinium Salts /
Eur. J. Org. Chem. 2011, 1280
Heteroaromatic Cation-Based Chromophores: Synthesis and Nonlinear Optical Properties of Alkynylazinium Salts /
Eur. J. Org. Chem. 2010, 6323
Application of Selective Palladium-Mediated Functionalization of the Pyrido%@5B3′,2′:4,5%@5Dpyrrolo%@5B1,2-c%@5Dpyrimidine Heterocyclic System for the Total Synthesis of Variolin B and Deoxyvariolin B /
Eur. J. Org. Chem. 2010, 5607
Novel Green Procedure for the Synthesis of 2-Arylbenzothiazoles Under Microwave Irradiation in Peg 200 Or Peg 400 /
Phosphorus, Sulfur, and Silicon and the Related Elements 2010, 185, 2292
Styryl dyes – synthesis and applications during the last 15 years /
Coloration Technology. 2010, 126, 55
An easy and fast ultrasonic selective S-alkylation of hetaryl thiols at room temperature /
Ultrasonics Sonochemistry 2010, 17, 783