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Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 04/2017, Volume 60, Issue 7, pp. 2819 - 2839
We previously reported the design of spirooxindoles with two identical substituents at the carbon-2 of the pyrrolidine core as potent MDM2 inhibitors. In this... 
TRIALS | ACTIVATION | DESIGN | CHEMISTRY, MEDICINAL | MECHANISM | DOCKING | PROTEIN-PROTEIN INTERACTION | FLUORINE | P53 PATHWAY | HIGHLY POTENT | RG7112 | Neoplasms - metabolism | Osteosarcoma - drug therapy | Bone and Bones - pathology | Leukemia - pathology | Humans | Antineoplastic Agents - therapeutic use | Leukemia - metabolism | Structure-Activity Relationship | Bone Neoplasms - pathology | Bone Neoplasms - metabolism | Bone and Bones - drug effects | Pyrrolidines - pharmacology | Pyrrolidines - therapeutic use | Bridged Bicyclo Compounds - chemistry | Bone and Bones - metabolism | Bridged Bicyclo Compounds - therapeutic use | Indoles - pharmacology | Antineoplastic Agents - pharmacokinetics | Antineoplastic Agents - pharmacology | Bone Neoplasms - drug therapy | Proto-Oncogene Proteins c-mdm2 - antagonists & inhibitors | Proto-Oncogene Proteins c-mdm2 - metabolism | Osteosarcoma - metabolism | Bridged Bicyclo Compounds - pharmacology | Pyrrolidines - pharmacokinetics | Leukemia - drug therapy | Rats | Antineoplastic Agents - chemistry | Drug Discovery | Pyrrolidines - chemistry | Neoplasms - drug therapy | Animals | Halogenation | Cell Line, Tumor | Indoles - pharmacokinetics | Indoles - therapeutic use | Mice | Molecular Docking Simulation | Bridged Bicyclo Compounds - pharmacokinetics | Neoplasms - pathology | Indoles - chemistry | Osteosarcoma - pathology | Index Medicus
Journal Article
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 02/2019, Volume 29, Issue 4, pp. 668 - 673
Parkinson’s disease is a relatively common neurological disorder with incidence increasing with age. Present treatments merely alleviate the symptoms and do... 
G2019S | LLE | Kinase inhibitor | Parkinson’s disease | Parkinson's disease | CHEMISTRY, MEDICINAL | G20198 | GENE | BRAIN-PENETRANT | CHEMISTRY, ORGANIC | PARKINSON-DISEASE | HIGHLY POTENT | MUTATIONS | Nervous system diseases
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 02/2019, Volume 29, Issue 4, pp. 674 - 680
The discovery of disease-modifying therapies for Parkinson’s Disease (PD) represents a critical need in neurodegenerative medicine. Genetic mutations in LRRK2... 
Brain penetration | Azaindazole | Kinase inhibitor | LRRK2 | Parkinson’s disease | Parkinson's disease | CHEMISTRY, MEDICINAL | CHEMISTRY, ORGANIC | MLI-2 | GENE | BRAIN-PENETRANT | HIGHLY POTENT | MUTATIONS | PARKINSONS-DISEASE | Brain research | Gene mutations | Neurons | Hydrogen | Analysis | Therapeutics | Permeability | Hydrogen bonding | Homeopathy | Materia medica and therapeutics
Journal Article
Journal Article
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 12/2018, Volume 61, Issue 24, pp. 11061 - 11073
A deconstruction of previously reported phosphoinositide 3-kinase delta (PI3K delta) inhibitors and subsequent regrowth led to the identification of a... 
TARGET | CHEMISTRY, MEDICINAL | EVOLUTION | SERIES | PI3K | PI3K-DELTA INHIBITORS | OPTIMIZATION | MECHANISMS | HIGHLY POTENT | LEAD
Journal Article
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, ISSN 0022-3565, 12/2015, Volume 355, Issue 3, pp. 397 - 409
Mutations in the leucine-rich repeat kinase 2 (LRRK2) gene are the most common genetic cause of familial and sporadic Parkinson's disease (PD). That the most... 
BRAIN PENETRANT | AUTOSOMAL-DOMINANT PARKINSONISM | GENE | DISEASE | PHARMACOLOGY & PHARMACY | HIGHLY POTENT | MUTATIONS | DISCOVERY
Journal Article
Proceedings of the National Academy of Sciences of the United States of America, ISSN 0027-8424, 7/2013, Volume 110, Issue 29, pp. 11698 - 11703
Highly active antiretroviral therapy (HAART) decreases plasma viremia below the limits of detection in the majority of HIV-infected individuals, thus serving... 
T lymphocytes | Highly active antiretroviral therapy | HIV | Cell lines | Lead | Viruses | Cell surface receptors | Phorbols | Acetates | HIV 1 | NF-?B | HIV latency | PKC-d | Bryostatin | PROTEIN-KINASE-C | ACTIVATION | PKC-delta | MULTIDISCIPLINARY SCIENCES | HOMALANTHUS-NUTANS | RESERVOIRS | NF-kappa B | 12-DEOXYPHORBOL | ACTIVE ANTIRETROVIRAL THERAPY | bryostatin | ERADICATION | PROVIDES | PHORBOL ESTER | HAART | Gene Expression Regulation, Viral - drug effects | Virus Activation - physiology | Magnetic Resonance Spectroscopy | Humans | Phorbol Esters - therapeutic use | Antigens, Differentiation, T-Lymphocyte - metabolism | Phorbol Esters - chemistry | Antigens, CD - metabolism | Phorbol Esters - chemical synthesis | Lectins, C-Type - metabolism | Flow Cytometry | Virus Activation - drug effects | Protein Kinase C - metabolism | Phorbol Esters - pharmacology | Protein Binding | HIV Infections - drug therapy | Molecular Structure | Antiretroviral Therapy, Highly Active - methods | CD4-Positive T-Lymphocytes - virology | Usage | Viremia | Physiological aspects | Genetic aspects | Properties | Drug therapy | T cells | HIV infection | Protein kinases | Lactones | Antiretroviral drugs | T cell receptors | Human immunodeficiency virus--HIV | Medical treatment | Index Medicus | Biological Sciences | NF-κB | Physical Sciences | PKC-δ
Journal Article