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Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression

Journal of medicinal chemistry, 2018-01, Vol.61 (2), p.462-481

2018

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Discovery of ERD-308 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Estrogen Receptor (ER)

Journal of medicinal chemistry, 2019-02, Vol.62 (3), p.1420-1442

2019

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Discovery of Novel Pyrrolo[2,3‑d]pyrimidine-based Derivatives as Potent JAK/HDAC Dual Inhibitors for the Treatment of Refractory Solid Tumors

Journal of medicinal chemistry, 2022-01, Vol.65 (2), p.1243-1264

2022

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Development of Protein Degradation Inducers of Androgen Receptor by Conjugation of Androgen Receptor Ligands and Inhibitor of Apoptosis Protein Ligands

Journal of medicinal chemistry, 2018-01, Vol.61 (2), p.543-575

2018

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Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein

Journal of medicinal chemistry, 2020-07, Vol.63 (14), p.7510-7528

2020

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Design, Synthesis, and Biological Evaluation of Novel Selenium-Containing Isocombretastatins and Phenstatins as Antitumor Agents

Journal of medicinal chemistry, 2017-09, Vol.60 (17), p.7300-7314

2017

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Organometallic Gold(III) Complexes Similar to Tetrahydroisoquinoline Induce ER-Stress-Mediated Apoptosis and Pro-Death Autophagy in A549 Cancer Cells

Journal of medicinal chemistry, 2018-04, Vol.61 (8), p.3478-3490

2018

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An Update on Poly(ADP-ribose)polymerase‑1 (PARP-1) Inhibitors: Opportunities and Challenges in Cancer Therapy

Journal of medicinal chemistry, 2016-11, Vol.59 (21), p.9575-9598

2016

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Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase

Journal of medicinal chemistry, 2016-05, Vol.59 (10), p.4948-4964

2016

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Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH)

Journal of medicinal chemistry, 2017-11, Vol.60 (22), p.9184-9204

2017

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Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy

Journal of medicinal chemistry, 2021-12, Vol.64 (24), p.18025-18053

2021

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Identification of (R)‑N‑((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)‑1H‑indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B‑Cell Lymphomas

Journal of medicinal chemistry, 2016-11, Vol.59 (21), p.9928-9941

2016

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Mitochondria-Targeted Lupane Triterpenoid Derivatives and Their Selective Apoptosis-Inducing Anticancer Mechanisms

Journal of medicinal chemistry, 2017-07, Vol.60 (14), p.6353-6363

2017

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Ado-trastuzumab Emtansine (T-DM1): An Antibody–Drug Conjugate (ADC) for HER2-Positive Breast Cancer

Journal of medicinal chemistry, 2014-08, Vol.57 (16), p.6949-6964

2014

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Design, Synthesis, and Biological Evaluation of Novel Selenium (Se-NSAID) Molecules as Anticancer Agents

Journal of medicinal chemistry, 2016-03, Vol.59 (5), p.1946-1959

2016

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Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer

Journal of medicinal chemistry, 2017-12, Vol.60 (24), p.9990-10012

2017

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DNA-Unresponsive Platinum(II) Complex Induces ERS-Mediated Mitophagy in Cancer Cells

Journal of medicinal chemistry, 2022-01, Vol.65 (1), p.520-530

2022

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Structure-Based Optimization of a Novel Class of Aldehyde Dehydrogenase 1A (ALDH1A) Subfamily-Selective Inhibitors as Potential Adjuncts to Ovarian Cancer Chemotherapy

Journal of medicinal chemistry, 2018-10, Vol.61 (19), p.8754-8773

2018

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Discovery of a Dual Tubulin and Poly(ADP-Ribose) Polymerase‑1 Inhibitor by Structure-Based Pharmacophore Modeling, Virtual Screening, Molecular Docking, and Biological Evaluation

Journal of medicinal chemistry, 2021-11, Vol.64 (21), p.15702-15715

2021

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Allosteric Inhibitors of SHP2 with Therapeutic Potential for Cancer Treatment

Journal of medicinal chemistry, 2017-12, Vol.60 (24), p.10205-10219

2017

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Pyrrolo[2′,3′:3,4]cyclohepta[1,2‑d][1,2]oxazoles, a New Class of Antimitotic Agents Active against Multiple Malignant Cell Types

Journal of medicinal chemistry, 2020-10, Vol.63 (20), p.12023-12042

2020

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Triazole–Dithiocarbamate Based Selective Lysine Specific Demethylase 1 (LSD1) Inactivators Inhibit Gastric Cancer Cell Growth, Invasion, and Migration

Journal of medicinal chemistry, 2013-11, Vol.56 (21), p.8543-8560

2013

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Discovery of an in Vivo Chemical Probe of the Lysine Methyltransferases G9a and GLP

Journal of medicinal chemistry, 2013-11, Vol.56 (21), p.8931-8942

2013

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Design, Synthesis, and Structure–Activity Relationship of Novel LSD1 Inhibitors Based on Pyrimidine–Thiourea Hybrids As Potent, Orally Active Antitumor Agents

Journal of medicinal chemistry, 2015-02, Vol.58 (4), p.1705-1716

2015

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Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression

Discovery of ERD-308 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Estrogen Receptor (ER)

Discovery of Novel Pyrrolo[2,3‑d]pyrimidine-based Derivatives as Potent JAK/HDAC Dual Inhibitors for the Treatment of Refractory Solid Tumors

Development of Protein Degradation Inducers of Androgen Receptor by Conjugation of Androgen Receptor Ligands and Inhibitor of Apoptosis Protein Ligands

Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein

Design, Synthesis, and Biological Evaluation of Novel Selenium-Containing Isocombretastatins and Phenstatins as Antitumor Agents

Organometallic Gold(III) Complexes Similar to Tetrahydroisoquinoline Induce ER-Stress-Mediated Apoptosis and Pro-Death Autophagy in A549 Cancer Cells

An Update on Poly(ADP-ribose)polymerase‑1 (PARP-1) Inhibitors: Opportunities and Challenges in Cancer Therapy

Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase

Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH)

Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy

Mitochondria-Targeted Lupane Triterpenoid Derivatives and Their Selective Apoptosis-Inducing Anticancer Mechanisms

Ado-trastuzumab Emtansine (T-DM1): An Antibody–Drug Conjugate (ADC) for HER2-Positive Breast Cancer

Design, Synthesis, and Biological Evaluation of Novel Selenium (Se-NSAID) Molecules as Anticancer Agents

Discovery of a Small-Molecule Bromodomain-Containing Protein 4 (BRD4) Inhibitor That Induces AMP-Activated Protein Kinase-Modulated Autophagy-Associated Cell Death in Breast Cancer

DNA-Unresponsive Platinum(II) Complex Induces ERS-Mediated Mitophagy in Cancer Cells

Structure-Based Optimization of a Novel Class of Aldehyde Dehydrogenase 1A (ALDH1A) Subfamily-Selective Inhibitors as Potential Adjuncts to Ovarian Cancer Chemotherapy

Discovery of a Dual Tubulin and Poly(ADP-Ribose) Polymerase‑1 Inhibitor by Structure-Based Pharmacophore Modeling, Virtual Screening, Molecular Docking, and Biological Evaluation

Allosteric Inhibitors of SHP2 with Therapeutic Potential for Cancer Treatment

Pyrrolo[2′,3′:3,4]cyclohepta[1,2‑d][1,2]oxazoles, a New Class of Antimitotic Agents Active against Multiple Malignant Cell Types

Triazole–Dithiocarbamate Based Selective Lysine Specific Demethylase 1 (LSD1) Inactivators Inhibit Gastric Cancer Cell Growth, Invasion, and Migration

Discovery of 7‑Methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro‑1H‑indol-5-yl)‑7H‑pyrrolo[2,3‑d]pyrimidin-4-amine (GSK2606414), a Potent and Selective First-in-Class Inhibitor of Protein Kinase R (PKR)-like Endoplasmic Reticulum Kinase (PERK)

Discovery of an in Vivo Chemical Probe of the Lysine Methyltransferases G9a and GLP

Design, Synthesis, and Structure–Activity Relationship of Novel LSD1 Inhibitors Based on Pyrimidine–Thiourea Hybrids As Potent, Orally Active Antitumor Agents

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