A03-Moléculas Bioactivas

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El grupo se dedica al diseño y síntesis de fármacos antitumorales. El estudio de las relaciones estructura-reactividad nos permite afinar las estructuras de los prototipos, incrementándose la actividad antiproliferativa y disminuyéndose la toxicidad.

Líneas de investigación

Estructuras homoquirales obtenidas a partir de bencenos disustituidos en posición orto, con actividad antitumoral
Nuevos compuestos con actividad antitumoral como inhibidores de colina quinasa

Palabras clave

Heterociclos de seis y siete miembros, fármacos antitumorales, purinas

ANDRES MARTINEZ MORENO

SOLEDAD ROMERO TAMUDO

JOAQUIN MARIA CAMPOS ROSA

ORCID

MERIEM CHAYAH GHADDAB

ORCID

MARIA DORA CARRION PEREGRINA

ANA CONEJO GARCIA

OLGA CRUZ LOPEZ

Inventores: ARANEGA JIMENEZ ANTONIA ; BOULAIZ HOURIA ; CAMPOS ROSA JOAQUIN MARIA ; CATIVIELA MARIN CARLOS ; CHOQUESILLO-LAZARTE DUANE; CONEJO GARCIA ANA ; CRUZ LOPEZ OLGA ; GARCIA CHAVES MARIA ANGEL ; GARCIA RUIZ JUAN MANUEL ; JIMENEZ SANZ ANA ISABEL; MARCHAL
Título: DIANAS BENZOHETEROEPINICOS
Código: P201030415

Inventores: Campos JM; Lopez l; Marchal JA; Boulaiz H; Aránega A; Gallo MA; Espinosa A; Rodríguez-Serrano F; Conejo, Ana
Título: NUEVAS (RS)- 7- O 9- (1,2,3,5- TETRAHIDRO-4,1-BENZOCAZEPIN-3-IL)-7H O9H-PURINAS CON ACTIVIDAD ANTITUMORAL
Código: P200802431

Inventores: ARANEGA JIMENEZ ANTONIA ; CAMPOS ROSA JOAQUIN ; ESPINOSA UBEDA ANTONIO ; GALLO MEZO MIGUEL ANGEL ; GOMEZ VIDAL JOSE ANTONIO ; NUNEZ CARRETERO M DEL CARMEN; MARCHAL CORRALES JUAN ANTONIO; Rodriguez-Serrano F ;
Título: (2,3-DIHIDRO-5H-1,4-BENZODIHETEROEPIN-3-IL)PURINAS CON ACTIVIDAD ANTITUMORAL
Código: P200601538

Espejo-Román, JM; Rubio-Ruiz, B; Chayah-Ghaddab, M; Vega-Gutierrez, C; García-García, G; Muguruza-Montero, A; Domene, C; Sánchez-Martín, RM; Cruz-López, O; Conejo-García, A

N-aryltetrahydroisoquinoline derivatives as HA-CD44 interaction inhibitors: Design, synthesis, computational studies, and antitumor effect

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2023;

FI:6,7; Q1

Bastos, RS; de Lima, LR; Neto, MFA; Yousaf, N; Cruz, JN; Campos, JM; Kimani, NM; Ramos, RS; Santos, CBR

Design and Identification of Inhibitors for the Spike-ACE2 Target of SARS-CoV-2

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, 2023;

FI:5,6; Q1

de Almeida, RBM; Barbosa, DB; do Bomfim, MR; Amparo, JAO; Andrade, BS; Costa, SL; Campos, JM; Cruz, JN; Santos, CBR; Leite, FHA; Botura, MB

Identification of a Novel Dual Inhibitor of Acetylcholinesterase and Butyrylcholinesterase: In Vitro and In Silico Studies

PHARMACEUTICALS, 2023;

FI:4,6; Q2

Santos, CBR; Lobato, CC; Ota, SSB; Silva, RC; Bittencourt, RCVS; Freitas, JJS; Ferreira, EFB; Ferreira, MB; Silva, RC; De Lima, AB; Campos, JM; Borges, RS; Bittencourt, JAHM

Analgesic Activity of 5-Acetamido-2-Hydroxy Benzoic Acid Derivatives and an In-Vivo and In-Silico Analysis of Their Target Interactions

PHARMACEUTICALS, 2023;

FI:4,6; Q2

Silva, LB; Ferreira, EFB; Maryam; Espejo-Román, JM; Costa, GV; Cruz, JV; Kimani, NM; Costa, JS; Bittencourt, JAHM; Cruz, JN; Campos, JM; Santos, CBR

Galantamine Based Novel Acetylcholinesterase Enzyme Inhibitors: A Molecular Modeling Design Approach

MOLECULES, 2023;

FI:4,6; Q2

Da Costa, GV; Neto, MFA; Da Silva, AKP; De Sa, EMF; Cancela, LCF; Vega, JS; Lobato, CM; Zuliani, JP; Espejo-Roman, JM; Campos, JM; Leite, FHA; Santos, CBR

Identification of Potential Insect Growth Inhibitor against Aedes aegypti: A Bioinformatics Approach

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, 2022;

FI:6,208; Q1

Espejo-Roman, JM; Rubio-Ruiz, B; Cano-Cortes, V; Cruz-Lopez, O; Gonzalez-Resines, S; Domene, C; Conejo-Garcia, A; Sanchez-Martin, RM

Selective Anticancer Therapy Based on a HA-CD44 Interaction Inhibitor Loaded on Polymeric Nanoparticles.

PHARMACEUTICS, 2022;

FI:6,525; Q1

Neto, MFA; Campos, JM; Cerqueira, APM; de Lima, LR; Da Costa, GV; Ramos, RD; Magalhaes, JT; Santos, CBR; Leite, FHA

Hierarchical Virtual Screening and Binding Free Energy Prediction of Potential Modulators of Aedes Aegypti Odorant-Binding Protein 1

MOLECULES, 2022;

FI:4,927; Q2

Cruz, JV; Rosa, JMC; Kimani, NM; Giuliatti, S; dos Santos, CBR

The Role of Celecoxib as a Potential Inhibitor in the Treatment of Inflammatory Diseases-A Review

CURRENT MEDICINAL CHEMISTRY, 2022;

FI:4,74; Q2

Arias, F; Camacho, ME; Carrion, MD

NMR spectroscopy study of new imidamide derivatives as nitric oxide synthase inhibitors

MAGNETIC RESONANCE IN CHEMISTRY, 2022;

FI:2,392; Q3

Cruz-Lopez, O; Ner, M; Nerin-Fonz, F; Jimenez-Martinez, Y; Araripe, D; Marchal, JA; Boulaiz, H; Gutierrez-de-Teran, H; Campos, JM; Conejo-Garcia, A

Design, synthesis, HER2 inhibition and anticancer evaluation of new substituted 1,5-dihydro-4,1-benzoxazepines

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2021;

FI:5,051; Q1

Lacal, JC; Zimmerman, T; Campos, JM

Choline Kinase: An Unexpected Journey for a Precision Medicine Strategy in Human Diseases

PHARMACEUTICS, 2021;

FI:6,321; Q1

Dias, AD; Dallemole, DR; Bruinsmann, FA; Silva, LFL; Cruz-Lopez, O; Conejo-Garcia, A; Battastini, AMO; Campos, JM; Guterres, SS; Pohlmann, AR; Figueiro, F

Development of bozepinib-loaded nanocapsules for nose-to-brain delivery: preclinical evaluation in glioblastoma

NANOMEDICINE, 2021;

FI:5,307; Q1

Ferreira, EFB; Silva, LB; Cruz, JV; Araujo, PHF; Kimani, NM; Leite, FHA; Campos, JM; Santos, CBR

An Overview of the alpha 4 beta 1 Integrin and the Potential Therapeutic Role of its Antagonists

CURRENT MEDICINAL CHEMISTRY, 2021;

FI:4,53; Q2

Santos, CBR; Santos, KLB; Cruz, JN; Leite, FHA; Borges, RS; Taft, CA; Campos, JM; Silva, CHTP

Molecular modeling approaches of selective adenosine receptor type 2A agonists as potential anti-inflammatory drugs

JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS, 2021;

FI:Not Available; Q4

de Andrade, P; Dias, AD; Figueiro, F; Torres, FC; Kawano, DF; Battastini, AMO; Carvalho, I; da Silva, CHTD; Campos, JM

1,2,3-Triazole tethered 2-mercaptobenzimidazole derivatives: design, synthesis and molecular assessment toward C6 glioma cell line

FUTURE MEDICINAL CHEMISTRY, 2020;

FI:3,607; Q2

Palheta, IC; Ferreira, LR; Vale, JKL; Silva, OPP; Herculano, AM; Oliveira, KRHM; Neto, AMJC; Campos, JM; Santos, CBR; Borges, RS

Alkylated Sesamol Derivatives as Potent Antioxidants

MOLECULES, 2020;

FI:3,267; Q2

dos Santos, KLB; Cruz, JN; Silva, LB; Ramos, RS; Neto, MFA; Lobato, CC; Ota, SSB; Leite, FHA; Borges, RS; da Silva, CHTP; Campos, JM; Santos, CBR

Identification of Novel Chemical Entities for Adenosine Receptor Type 2A Using Molecular Modeling Approaches

MOLECULES, 2020;

FI:3,267; Q2

Araujo, PHF; Ramos, RS; da Cruz, JN; Silva, SG; Ferreira, EFB; de Lima, LR; Macedo, WJC; Espejo-Roman, JM; Campos, JM; Santos, CBR

Identification of Potential COX-2 Inhibitors for the Treatment of Inflammatory Diseases Using Molecular Modeling Approaches

MOLECULES, 2020;

FI:3,267; Q2

Romagnoli, R; Oliva, P; Salvador, MK; Camacho, ME; Padroni, C; Brancale, A; Ferla, S; Hamel, E; Ronca, R; Grillo, E; Bortolozzi, R; Rruga, F; Mariotto, E; Viola, G

Design, synthesis and biological evaluation of novel vicinal diaryl-substituted 1H-Pyrazole analogues of combretastatin A-4 as highly potent tubulin polymerization inhibitors

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2019;

FI:4,833; D1

Bittencourt, JAHM; Neto, MFA; Lacerda, PS; Bittencourt, RCVS; Silva, RC; Lobato, CC; Silva, LB; Leite, FHA; Zuliani, JP; Rosa, JMC; Borges, RS; Santos, CBR

In Silico Evaluation of Ibuprofen and Two Benzoylpropionic Acid Derivatives with Potential Anti-Inflammatory Activity

MOLECULES, 2019;

FI:3,06; Q2

Borges, RS; Palheta, IC; Ota, SSB; Morais, RB; Barros, VA; Ramos, RS; Silva, RC; Costa, JD; Silva, CHTP; Campos, JM; Santos, CBR

Toward of Safer Phenylbutazone Derivatives by Exploration of Toxicity Mechanism

MOLECULES, 2019;

FI:3,06; Q2

Ferreira, EFB; Silva, LB; Costa, GV; Costa, JS; Fujishima, MAT; Leao, RP; Ferreira, ALS; Federico, LB; Silva, CHTP; Rosa, JMC; Macedo, WJC; Santos, CBR

Identification of New Inhibitors with Potential Antitumor Activity from Polypeptide Structures via Hierarchical Virtual Screening

MOLECULES, 2019;

FI:3,06; Q2

Fernandez-Saez, N; Campos, JM; Camacho, ME; Carrion, MD

NMR studies of new heterocycles tethered to purine moieties with anticancer activity

MAGNETIC RESONANCE IN CHEMISTRY, 2019;

FI:1,731; Q3

Ramirez, A; Conejo-Garcia, A; Grinan-Lison, C; Lopez-Cara, LC; Jimenez, G; Campos, JM; Marchal, JA; Boulaiz, H

Enhancement of Tumor Cell Death by Combining gef Gene Mediated Therapy and New 1,4-Benzoxazepin-2,6-Dichloropurine Derivatives in Breast Cancer Cells

FRONTIERS IN PHARMACOLOGY, 2018;

FI:3,831; Q1

Del Ponte, G; Archanjo, FC; Watanabe, LY; Donate, PM; Campos, JM

Syntheses of non-aromatic medium and large rings synthesized via phenylnitrenium ions

ARABIAN JOURNAL OF CHEMISTRY, 2018;

FI:2,969; Q2

Mahfoudh, N; Marin-Ramos, NI; Gil, AM; Jimenez, AI; Choquesillo-Lazarte, D; Kawano, DF; Campos, JM; Cativiela, C

Cysteine-based 3-substituted 1,5-benzoxathiepin derivatives: Two new classes of anti-proliferative agents

ARABIAN JOURNAL OF CHEMISTRY, 2018;

FI:2,969; Q2

Gonzalez-Martinez, D; Fernandez-Saez, N; Cativiela, C; Campos, JM; Gotor-Fernandez, V

Development of Biotransamination Reactions towards the 3,4-Dihydro-2H-1,5-benzoxathiepin-3-amine Enantiomers

CATALYSTS, 2018;

FI:3,465; Q2

Costa, JD; Ramos, RD; Costa, KDL; Brasil, DDB; da Silva, CHTD; Ferreira, EFB; Borges, RD; Campos, JM; Macedo, WJD; dos Santos, CBR

An In Silico Study of the Antioxidant Ability for Two Caffeine Analogs Using Molecular Docking and Quantum Chemical Methods

MOLECULES, 2018;

FI:3,098; Q2

Cruz-Lopez, O; Ramirez, A; Navarro, SA; Garcia, MA; Marchal, JA; Campos, JM; Conejo-Garcia, A

1-(Benzenesulfonyl)-1,5-dihydro-4,1-benzoxazepine as a new scaffold for the design of antitumor compounds

FUTURE MEDICINAL CHEMISTRY, 2017;

FI:3,556; Q1

Morales, F; Ramirez, A; Morata-Tarifa, C; Navarro, SA; Marchal, JA; Campos, JM; Conejo-Garcia, A

Antitumoral activity of 1,2-diaminocyclohexane derivatives in breast, colon and skin human cancer cells

FUTURE MEDICINAL CHEMISTRY, 2017;

FI:3,556; Q1

Camacho, ME; Carrion, MD; Chayah, M; Campos, JM

The use of wiki to promote students’ learning in higher education (Degree in Pharmacy)

INTERNATIONAL JOURNAL OF EDUCATIONAL TECHNOLOGY IN HIGHER EDUCATION, 2016;

Serran-Aguilera, L; Denton, H; Rubio-Ruiz, B; Lopez-Gutierrez, B; Entrena, A; Izquierdo, L; Smith, TK; Conejo-Garcia, A; Hurtado-Guerrero, R

Plasmodium falciparum Choline Kinase Inhibition Leads to a Major Decrease in Phosphatidylethanolamine Causing Parasite Death

SCIENTIFIC REPORTS, 2016;

FI:5,228; Q1

Garcia-Rubino, ME; Lozano-Lopez, C; Campos, JM

Inhibitors of Cancer Stem Cells

ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY, 2016;

FI:2,722; Q2

Gonzalez-Perez, JM; Choquesillo-Lazarte, D; Dominguez-Martin, A; Vilchez-iodriguez, E; Perez-Toro, I; Castineiras, A; Arriortua, OK; Garcia-Rubino, ME; Matilla-Hernandez, A; Niclos-Gutierrez, J

Metal binding pattern of acyclovir in ternary copper(II) complexes having an S-thioether or S-disulfide NO2S-tripodal tetradentate chelator

INORGANICA CHIMICA ACTA, 2016;

FI:1,918; Q2

Morales, F; Campos, JM; Conejo-Garcia, A

H-1 and C-13 NMR spectral data of p-nitrobenzenesulfonamides and dansylsulfonamides derived from N-alkylated o-(purinemethyl)anilines

MAGNETIC RESONANCE IN CHEMISTRY, 2016;

FI:1,226; Q3

Torres, FC; Garcia-Rubino, ME; Lozano-Lopez, C; Kawano, DF; Eifler-Lima, VL; von Poser, GL; Campos, JM

Imidazoles and Benzimidazoles as Tubulin-Modulators for Anti-Cancer Therapy

CURRENT MEDICINAL CHEMISTRY, 2015;

FI:3,853; D1

Gomez-Perez, V; Manzano, JI; Garcia-Hernandez, R; Castanys, S; Gamarro, F; Campos, JM

Design, synthesis and anti-leishmanial activity of novel symmetrical bispyridinium cyclophanes

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2015;

FI:3,447; Q1

Morales, F; Conejo-Garcia, A; Ramirez, A; Morata, C; Marchal, JA; Campos, JM

p-Nitrobenzenesulfonamides and their fluorescent dansylsulfonamides derived from N-alkylated o-(purine-methyl)anilines as novel antitumour agents

RSC ADVANCES, 2015;

FI:3,84; Q1

Lacal, JC; Campos, JM

Preclinical Characterization of RSM-932A, a Novel Anticancer Drug Targeting the Human Choline Kinase Alpha, an Enzyme Involved in Increased Lipid Metabolism of Cancer Cells

MOLECULAR CANCER THERAPEUTICS, 2015;

FI:5,683; Q1

Gonzalez-Perez, JM; Choquesillo-Lazarte, D; Dominguez-Martin, A; El Bakkali, H; Garcia-Rubino, ME; Perez-Toro, I; Vilchez-Rodriguez, E; Castineiras, A; Nurchi, VM; Niclos-Gutierrez, J