List of works - Joaquín Pastor

A General and Highly Efficient Solid Phase Synthesis of Oligosaccharides. Total Synthesis of a Heptasaccharide Phytoalexin Elicitor (HPE)

article by K. C. Nicolaou et al published January 1997 in Journal of the American Chemical Society

A cell-based screen identifies ATR inhibitors with synthetic lethal properties for cancer-associated mutations.

scientific article published on 8 May 2011

A clinically compatible drug-screening platform based on organotypic cultures identifies vulnerabilities to prevent and treat brain metastasis

scientific article published on 17 February 2022

A novel phosphatidylinositol 3-kinase (PI3K) inhibitor directs a potent FOXO-dependent, p53-independent cell cycle arrest phenotype characterized by the differential induction of a subset of FOXO-regulated genes

scientific article

Alternative Activation Mechanisms of Protein Kinase B Trigger Distinct Downstream Signaling Responses

scientific article

Anti-tumor effects of PIM/PI3K/mTOR triple kinase inhibitor IBL-302 in neuroblastoma

scientific article published on 01 January 2020

Assessment of additive/nonadditive effects in structure-activity relationships: implications for iterative drug design

scientific article

Azino-Fused Benzimidazolium Salts as DNA Intercalating Agents. 2

Biological characterization of ETP-46321 a selective and efficacious inhibitor of phosphoinositide-3-kinases.

scientific article published on 24 May 2012

Design and synthesis of a series of piperazine-1-carboxamidine derivatives with antifungal activity resulting from accumulation of endogenous reactive oxygen species.

scientific article

Dihydrothiazolopyridone derivatives as a novel family of positive allosteric modulators of the metabotropic glutamate 5 (mGlu5) receptor

scientific article published on 04 September 2013

Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity

scientific article

Discovery of a potent, selective, and orally active phosphodiesterase 10A inhibitor for the potential treatment of schizophrenia

scientific article

Discovery of mitogen-activated protein kinase-interacting kinase 1 inhibitors by a comprehensive fragment-oriented virtual screening approach.

scientific article

Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors

scientific article published on 19 February 2019

ETP-46321, a dual p110α/δ class IA phosphoinositide 3-kinase inhibitor modulates T lymphocyte activation and collagen-induced arthritis.

scientific article published on 13 February 2016

Fragment-hopping-based discovery of a novel chemical series of proto-oncogene PIM-1 kinase inhibitors

scientific article

Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy.

scientific article published on 2 April 2017

Hit to lead evaluation of 1,2,3-triazolo[4,5-b]pyridines as PIM kinase inhibitors

scientific article

Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor.

scientific article

Identification of novel PI3K inhibitors through a scaffold hopping strategy.

scientific article

Imidazo[1,2-a]pyrazines as novel PI3K inhibitors

scientific article published on 28 January 2012

Inhibition of TRF1 Telomere Protein Impairs Tumor Initiation and Progression in Glioblastoma Mouse Models and Patient-Derived Xenografts

scientific article published in November 2017

Non-genotoxic activation of p53 through the RPL11-dependent ribosomal stress pathway.

scientific article published on 24 October 2014

Optimizing the performance of in silico ADMET general models according to local requirements: MARS approach. solubility estimations as case study.

scientific article

PI3Kα inhibition reduces obesity in mice

scientific article (publication date: 4 November 2016)

Pharmacological inhibition of PI3K reduces adiposity and metabolic syndrome in obese mice and rhesus monkeys.

scientific article

Pim 1 kinase inhibitor ETP-45299 suppresses cellular proliferation and synergizes with PI3K inhibition

scientific article published on 3 November 2010

Polymer-supported selenium reagents for organic synthesis

article

Preclinical evaluation of a novel triple-acting PIM/PI3K/mTOR inhibitor, IBL-302, in breast cancer

scientific article published on 10 February 2020

Pten positively regulates brown adipose function, energy expenditure, and longevity

scientific article

RAB7 counteracts PI3K-driven macropinocytosis activated at early stages of melanoma development

scientific article

Rapid identification of ETP-46992, orally bioavailable PI3K inhibitor, selective versus mTOR.

scientific article

Screening protocol for the identification of modulators by immunofluorescent cell-based assay

scientific article published on 20 September 2019

Solid Phase Synthesis of Macrocycles by an Intramolecular Ketophosphonate Reaction. Synthesis of a (dl)-Muscone Library

scientific article published in 1998

Solid-Phase Synthesis of Macrocyclic Systems by a Cyclorelease Strategy: Application of the Stille Coupling to a Synthesis of (S)-Zearalenone.

scientific article published in October 1998

Synthesis of 3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazoles, displaying combined 5-HT uptake inhibiting and alpha(2)-adrenoceptor antagonistic activities: a novel series of potential antidepressants

scientific article published in August 2003

Synthesis of 3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazoles, displaying combined 5-HT uptake inhibiting and alpha2-adrenoceptor antagonistic activities. Part 2: Further exploration on the cinnamyl moiety

scientific article

Synthesis of new azino fused benzimidazolium salts. a new family of DNA intercalating agents. I

article published in 1995

The targetable kinase PIM1 drives ALK inhibitor resistance in high-risk neuroblastoma independent of MYCN status

scientific article published on 28 November 2019

Therapeutic inhibition of TRF1 impairs the growth of p53-deficient K-RasG12V-induced lung cancer by induction of telomeric DNA damage

scientific article published on 13 May 2015

Tissue damage and senescence provide critical signals for cellular reprogramming in vivo.

scientific article

Tricyclic isoxazolines: Identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and α2-adrenoceptor antagonism

scientific article published on 21 March 2007

List of works by Joaquín Pastor

A General and Highly Efficient Solid Phase Synthesis of Oligosaccharides. Total Synthesis of a Heptasaccharide Phytoalexin Elicitor (HPE)

A cell-based screen identifies ATR inhibitors with synthetic lethal properties for cancer-associated mutations.

A clinically compatible drug-screening platform based on organotypic cultures identifies vulnerabilities to prevent and treat brain metastasis

A novel phosphatidylinositol 3-kinase (PI3K) inhibitor directs a potent FOXO-dependent, p53-independent cell cycle arrest phenotype characterized by the differential induction of a subset of FOXO-regulated genes

Alternative Activation Mechanisms of Protein Kinase B Trigger Distinct Downstream Signaling Responses

Anti-tumor effects of PIM/PI3K/mTOR triple kinase inhibitor IBL-302 in neuroblastoma

Assessment of additive/nonadditive effects in structure-activity relationships: implications for iterative drug design

Azino-Fused Benzimidazolium Salts as DNA Intercalating Agents. 2

Biological characterization of ETP-46321 a selective and efficacious inhibitor of phosphoinositide-3-kinases.

Design and synthesis of a series of piperazine-1-carboxamidine derivatives with antifungal activity resulting from accumulation of endogenous reactive oxygen species.

Dihydrothiazolopyridone derivatives as a novel family of positive allosteric modulators of the metabotropic glutamate 5 (mGlu5) receptor

Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity

Discovery of a potent, selective, and orally active phosphodiesterase 10A inhibitor for the potential treatment of schizophrenia

Discovery of mitogen-activated protein kinase-interacting kinase 1 inhibitors by a comprehensive fragment-oriented virtual screening approach.

Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors

ETP-46321, a dual p110α/δ class IA phosphoinositide 3-kinase inhibitor modulates T lymphocyte activation and collagen-induced arthritis.

Fragment-hopping-based discovery of a novel chemical series of proto-oncogene PIM-1 kinase inhibitors

Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy.

Hit to lead evaluation of 1,2,3-triazolo[4,5-b]pyridines as PIM kinase inhibitors

Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor.

Identification of novel PI3K inhibitors through a scaffold hopping strategy.

Imidazo[1,2-a]pyrazines as novel PI3K inhibitors

Inhibition of TRF1 Telomere Protein Impairs Tumor Initiation and Progression in Glioblastoma Mouse Models and Patient-Derived Xenografts

Non-genotoxic activation of p53 through the RPL11-dependent ribosomal stress pathway.

Optimizing the performance of in silico ADMET general models according to local requirements: MARS approach. solubility estimations as case study.

PI3Kα inhibition reduces obesity in mice

Pharmacological inhibition of PI3K reduces adiposity and metabolic syndrome in obese mice and rhesus monkeys.

Pim 1 kinase inhibitor ETP-45299 suppresses cellular proliferation and synergizes with PI3K inhibition

Polymer-supported selenium reagents for organic synthesis

Preclinical evaluation of a novel triple-acting PIM/PI3K/mTOR inhibitor, IBL-302, in breast cancer

Pten positively regulates brown adipose function, energy expenditure, and longevity

RAB7 counteracts PI3K-driven macropinocytosis activated at early stages of melanoma development

Rapid identification of ETP-46992, orally bioavailable PI3K inhibitor, selective versus mTOR.

Screening protocol for the identification of modulators by immunofluorescent cell-based assay

Solid Phase Synthesis of Macrocycles by an Intramolecular Ketophosphonate Reaction. Synthesis of a (dl)-Muscone Library

Solid-Phase Synthesis of Macrocyclic Systems by a Cyclorelease Strategy: Application of the Stille Coupling to a Synthesis of (S)-Zearalenone.

Synthesis of 3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazoles, displaying combined 5-HT uptake inhibiting and alpha(2)-adrenoceptor antagonistic activities: a novel series of potential antidepressants

Synthesis of 3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazoles, displaying combined 5-HT uptake inhibiting and alpha2-adrenoceptor antagonistic activities. Part 2: Further exploration on the cinnamyl moiety

Synthesis of new azino fused benzimidazolium salts. a new family of DNA intercalating agents. I

The targetable kinase PIM1 drives ALK inhibitor resistance in high-risk neuroblastoma independent of MYCN status

Therapeutic inhibition of TRF1 impairs the growth of p53-deficient K-RasG12V-induced lung cancer by induction of telomeric DNA damage

Tissue damage and senescence provide critical signals for cellular reprogramming in vivo.

Tricyclic isoxazolines: Identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and α2-adrenoceptor antagonism

Unexpected NC bond fission of fused N-alkylbenzimidazolium salts. A new approach to pyrido[1,2-a]- or pyridazino[1,6-a]benzimidazoles