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Buparlisib in Patients With Recurrent Glioblastoma Harboring Phosphatidylinositol 3-Kinase Pathway Activation: An Open-Label, Multicenter, Multi-Arm, Phase II Trial

Journal of clinical oncology, 2019-03, Vol.37 (9), p.741-750

2019

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Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective

Journal of medicinal chemistry, 2019-05, Vol.62 (10), p.4815-4850

2019

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Discovery and Optimization of Pyridazinones as PI3Kδ Selective Inhibitors for Administration by Inhalation

Journal of medicinal chemistry, 2024-07, Vol.67 (13), p.11103-11124

2024

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Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases

Journal of medicinal chemistry, 2019-05, Vol.62 (10), p.4783-4814

2019

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Discovery of Pyrazolo[1,5- a ]pyridine Derivatives as Potent and Selective PI3Kγ/δ Inhibitors

Journal of medicinal chemistry, 2024-09, Vol.67 (17), p.15199-15219

2024

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Development of PI3K inhibitors: Advances in clinical trials and new strategies (Review)

Pharmacological research, 2021-11, Vol.173, p.105900-105900, Article 105900

2021

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Discovery of Potent and Selective PI3Kγ Inhibitors

Journal of medicinal chemistry, 2020-10, Vol.63 (19), p.11235-11257

2020

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Small-molecule inhibitors of breast cancer-related targets: Potential therapeutic agents for breast cancer

European journal of medicinal chemistry, 2021-01, Vol.210, p.112954-112954, Article 112954

2021

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Designing Small Molecule PI3Kγ Inhibitors: A Review of Structure-Based Methods and Computational Approaches

Journal of medicinal chemistry, 2024-07, Vol.67 (13), p.10530-10547

2024

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Structure-Based Drug Design and Synthesis of PI3Kα-Selective Inhibitor (PF-06843195)

Journal of medicinal chemistry, 2021-01, Vol.64 (1), p.644-661

2021

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Molecular design of dual inhibitors of PI3K and potential molecular target of cancer for its treatment: A review

European journal of medicinal chemistry, 2022-01, Vol.228, p.114039-114039, Article 114039

2022

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Properties of FDA-approved small molecule phosphatidylinositol 3-kinase inhibitors prescribed for the treatment of malignancies

Pharmacological research, 2021-06, Vol.168, p.105579-105579, Article 105579

Roskoski, Robert

2021

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Discovery of a Potent and Selective PI3Kδ Inhibitor ( S )-2,4-Diamino-6-((1-(7-fluoro-1-(4-fluorophenyl)-4-oxo-3-phenyl-4 H -quinolizin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile with Improved Pharmacokinetic Profile and Superior Efficacy in Hematological Cancer Models

Journal of medicinal chemistry, 2020-12, Vol.63 (23), p.14700-14723

2020

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Translation of Inhaled Drug Optimization Strategies into Clinical Pharmacokinetics and Pharmacodynamics Using GSK2292767A, a Novel Inhaled Phosphoinositide 3-Kinase δ Inhibitor

The Journal of pharmacology and experimental therapeutics, 2019-06, Vol.369 (3), p.443-453

2019

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From lab to clinic: The discovery and optimization journey of PI3K inhibitors

European journal of medicinal chemistry, 2024-11, Vol.277, p.116786, Article 116786

2024

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Phase Ib study of the MEK inhibitor cobimetinib (GDC-0973) in combination with the PI3K inhibitor pictilisib (GDC-0941) in patients with advanced solid tumors

Investigational new drugs, 2020-04, Vol.38 (2), p.419-432

2020

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Phase I trial of copanlisib, a selective PI3K inhibitor, in combination with cetuximab in patients with recurrent and/or metastatic head and neck squamous cell carcinoma

Investigational new drugs, 2021-12, Vol.39 (6), p.1641-1648

2021

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Managing toxicities of phosphatidylinositol-3-kinase (PI3K) inhibitors

Hematology, 2020-12, Vol.2020 (1), p.346-356

2020

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Discovery of GSK251: A Highly Potent, Highly Selective, Orally Bioavailable Inhibitor of PI3Kδ with a Novel Binding Mode

Journal of medicinal chemistry, 2021-09, Vol.64 (18), p.13780-13792

2021

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Folate decorated polymeric micelles for targeted delivery of the kinase inhibitor dactolisib to cancer cells

International journal of pharmaceutics, 2020-05, Vol.582, p.119305, Article 119305

2020

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SGLT2 inhibition improves PI3Kα inhibitor–induced hyperglycemia: findings from preclinical animal models and from patients in the BYLieve and SOLAR-1 trials

Breast cancer research and treatment, 2024-11, Vol.208 (1), p.111-121

2024

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Design, Synthesis, and Pharmacological Evaluation of First‐in‐Class Multitarget N‐Acylhydrazone Derivatives as Selective HDAC6/8 and PI3Kα Inhibitors

ChemMedChem, 2020-03, Vol.15 (6), p.539-551

2020

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Design, synthesis, and biological evaluation of novel 6-(pyridin-3-yl) quinazolin-4(3H)-one derivatives as potential anticancer agents via PI3K inhibition

Bioorganic & medicinal chemistry, 2021-09, Vol.46, p.116346-116346, Article 116346

2021

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Structural effects of morpholine replacement in ZSTK474 on Class I PI3K isoform inhibition: Development of novel MEK/PI3K bifunctional inhibitors

European journal of medicinal chemistry, 2022-02, Vol.229, p.113996-113996, Article 113996

2022

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Relationship between Pharmacokinetics and Pharmacodynamic Responses in Healthy Smokers Informs a Once-Daily Dosing Regimen for Nemiralisib

The Journal of pharmacology and experimental therapeutics, 2019-06, Vol.369 (3), p.337-344

2019

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Buparlisib in Patients With Recurrent Glioblastoma Harboring Phosphatidylinositol 3-Kinase Pathway Activation: An Open-Label, Multicenter, Multi-Arm, Phase II Trial

Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective

Discovery and Optimization of Pyridazinones as PI3Kδ Selective Inhibitors for Administration by Inhalation

Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases

Discovery of Pyrazolo[1,5- a ]pyridine Derivatives as Potent and Selective PI3Kγ/δ Inhibitors

Development of PI3K inhibitors: Advances in clinical trials and new strategies (Review)

Discovery of Potent and Selective PI3Kγ Inhibitors

Small-molecule inhibitors of breast cancer-related targets: Potential therapeutic agents for breast cancer

Designing Small Molecule PI3Kγ Inhibitors: A Review of Structure-Based Methods and Computational Approaches

Structure-Based Drug Design and Synthesis of PI3Kα-Selective Inhibitor (PF-06843195)

Molecular design of dual inhibitors of PI3K and potential molecular target of cancer for its treatment: A review

Properties of FDA-approved small molecule phosphatidylinositol 3-kinase inhibitors prescribed for the treatment of malignancies

Discovery of a Potent and Selective PI3Kδ Inhibitor ( S )-2,4-Diamino-6-((1-(7-fluoro-1-(4-fluorophenyl)-4-oxo-3-phenyl-4 H -quinolizin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile with Improved Pharmacokinetic Profile and Superior Efficacy in Hematological Cancer Models

Translation of Inhaled Drug Optimization Strategies into Clinical Pharmacokinetics and Pharmacodynamics Using GSK2292767A, a Novel Inhaled Phosphoinositide 3-Kinase δ Inhibitor

From lab to clinic: The discovery and optimization journey of PI3K inhibitors

Phase Ib study of the MEK inhibitor cobimetinib (GDC-0973) in combination with the PI3K inhibitor pictilisib (GDC-0941) in patients with advanced solid tumors

Phase I trial of copanlisib, a selective PI3K inhibitor, in combination with cetuximab in patients with recurrent and/or metastatic head and neck squamous cell carcinoma

Managing toxicities of phosphatidylinositol-3-kinase (PI3K) inhibitors

Discovery of GSK251: A Highly Potent, Highly Selective, Orally Bioavailable Inhibitor of PI3Kδ with a Novel Binding Mode

Folate decorated polymeric micelles for targeted delivery of the kinase inhibitor dactolisib to cancer cells

SGLT2 inhibition improves PI3Kα inhibitor–induced hyperglycemia: findings from preclinical animal models and from patients in the BYLieve and SOLAR-1 trials

Design, Synthesis, and Pharmacological Evaluation of First‐in‐Class Multitarget N‐Acylhydrazone Derivatives as Selective HDAC6/8 and PI3Kα Inhibitors

Design, synthesis, and biological evaluation of novel 6-(pyridin-3-yl) quinazolin-4(3H)-one derivatives as potential anticancer agents via PI3K inhibition

Structural effects of morpholine replacement in ZSTK474 on Class I PI3K isoform inhibition: Development of novel MEK/PI3K bifunctional inhibitors

Relationship between Pharmacokinetics and Pharmacodynamic Responses in Healthy Smokers Informs a Once-Daily Dosing Regimen for Nemiralisib

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