1,4,5,6-Tetrahydropyrrolo[3,4-<i>c</i>]pyrazoles:  Identification of a Potent Aurora Kinase Inhibitor with a Favorable Antitumor Kinase Inhibition Profile

Daniele Fancelli, Jürgen Moll, Mario Varasi, +22

Journal of Medicinal Chemistry

Molecular PharmacologyMedicinal ChemistryChemoprevention StrategyBiochemistryVivo Tumor Models +12

Potent and Selective Aurora Inhibitors Identified by the Expansion of a Novel Scaffold for Protein Kinase Inhibition

Daniele Fancelli, Daniela Berta, Simona Bindi, +20

Journal of Medicinal Chemistry

Molecular BiologyChemical BiologyPharmaceutical ChemistryTumor BiologyMedicinal Chemistry +16

Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1<i>H</i>-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy

Gianluca Papeo, Helena Posteri, Daniela Borghi, +26

Journal of Medicinal Chemistry

Cancer TherapyDrug TargetPharmacotherapyParp-1 Selective InhibitorChemical Biology +16

Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis

Beatriz Baragaña, Barbara Forte, Ryan Choi, +74

Proceedings of the National Academy of Sciences

NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor

Italo Beria, R Bossi, Maria Gabriella Brasca, +12

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryBiochemistryMedicineNatural SciencesMechanism Of Action +7

Prioritization of Molecular Targets for Antimalarial Drug Discovery

Barbara Forte, Sabine Ottilie, Andrew Plater, +17

ACS Infectious Diseases

First Cdc7 Kinase Inhibitors: Pyrrolopyridinones as Potent and Orally Active Antitumor Agents. 2. Lead Discovery

Maria Menichincheri, Alberto Bargiotti, Jens Berthelsen, +28

Journal of Medicinal Chemistry

Molecular BiologyPharmacotherapyCell CycleTumor BiologyMolecular Pharmacology +15

Cdc7 Kinase Inhibitors: 5-Heteroaryl-3-Carboxamido-2-Aryl Pyrroles as Potential Antitumor Agents. 1. Lead Finding

Maria Menichincheri, Clara Albanese, Cristina Alli, +33

Journal of Medicinal Chemistry

Compound 18Lead IdentificationPharmaceutical ChemistryTumor BiologyMolecular Pharmacology +17

Biochemical and Structural Characterization of Selective Allosteric Inhibitors of the <i>Plasmodium falciparum</i> Drug Target, Prolyl-tRNA-synthetase

Stephen N. Hewitt, David M. Dranow, Benjamin G. Horst, +23

ACS Infectious Diseases

Structural CharacterizationDrug TargetBioorganic ChemistryAntiparasitic AgentMalaria +16

Structural Insight into Maternal Embryonic Leucine Zipper Kinase (MELK) Conformation and Inhibition toward Structure-Based Drug Design

Giulia Canevari, Stefania Re Depaolini, Ulisse Cucchi, +6

Biochemistry

Drug TargetMolecular BiologyStructural InsightMelk InhibitorsTumor Biology +14