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Recent progress on third generation covalent EGFR inhibitors

Bioorganic & medicinal chemistry letters, 2016-04, Vol.26 (8), p.1861-1868

2016

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Design and synthesis of a novel pyrrolidinyl pyrido pyrimidinone derivative as a potent inhibitor of PI3Kα and mTOR

Bioorganic & medicinal chemistry letters, 2012-08, Vol.22 (15), p.5098-5103

2012

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Precedence and Promise of Covalent Inhibitors of EGFR and KRAS for Patients with Non-Small-Cell Lung Cancer

ACS medicinal chemistry letters, 2018-09, Vol.9 (9), p.861-863

2018

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The development and SAR of pyrrolidine carboxamide 11β-HSD1 inhibitors

Bioorganic & medicinal chemistry letters, 2010-05, Vol.20 (9), p.2897-2902

2010

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Quinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors

Bioorganic & medicinal chemistry letters, 2011-02, Vol.21 (4), p.1270-1274

2011

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Targeting the mTOR pathway in tumor malignancy

Current cancer drug targets, 2013-03, Vol.13 (3), p.267

2013

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4-Methylpteridinones as orally active and selective PI3K/mTOR dual inhibitors

Bioorganic & medicinal chemistry letters, 2010-10, Vol.20 (20), p.6096-6099

2010

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The pharmacologic and toxicologic characterization of the potent and selective KRAS G12D inhibitors ERAS-4693 and ERAS-5024

Toxicology and applied pharmacology, 2023-09, Vol.474, p.116601-116601, Article 116601

2023

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5-Heteroatom substituted pyrazoles as canine COX-2 inhibitors. Part III: Molecular modeling studies on binding contribution of 1-(5-methylsulfonyl)pyrid-2-yl and 4-nitrile

Bioorganic & medicinal chemistry letters, 2007-02, Vol.17 (4), p.1067-1072

2007

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5-Heteroatom substituted pyrazoles as canine COX-2 inhibitors. Part 1: Structure–activity relationship studies of 5-alkylamino pyrazoles and discovery of a potent, selective, and orally active analog

Bioorganic & medicinal chemistry letters, 2006-01, Vol.16 (2), p.288-292

2006

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Comparative structure–activity relationship studies of 1-(5-methylsulfonylpyrid-2-yl)-5-alkyl and (hetero)aryl triazoles and pyrazoles in canine COX inhibition

Bioorganic & medicinal chemistry, 2008-02, Vol.18 (3), p.1042-1045

2008

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Synthesis and SAR of heteroaryl-phenyl-substituted pyrazole derivatives as highly selective and potent canine COX-2 inhibitors

Bioorganic & medicinal chemistry letters, 2006-04, Vol.16 (8), p.2076-2080

2006

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PF-04691502, a potent and selective oral inhibitor of PI3K and mTOR kinases with antitumor activity

Molecular cancer therapeutics, 2011-11, Vol.10 (11), p.2189-2199

2011

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5-Heteroatom-substituted pyrazoles as canine COX-2 inhibitors: Part 2. Structure–activity relationship studies of 5-alkylethers and 5-thioethers

Bioorganic & medicinal chemistry letters, 2006-03, Vol.16 (5), p.1202-1206

2006

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Discovery of N‑((3R,4R)‑4-Fluoro-1-(6-((3-methoxy-1-methyl‑1H‑pyrazol-4-yl)amino)-9-methyl‑9H‑purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR

Journal of medicinal chemistry, 2017-04, Vol.60 (7), p.3002-3019

2017

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Structure-Based Design and Synthesis of Potent and Selective KRAS G12D Inhibitors

ACS medicinal chemistry letters, 2023-10, Vol.14 (10), p.1351-1357

2023

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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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Discovery of 1‑{(3R,4R)‑3-[({5-Chloro-2-[(1-methyl‑1H‑pyrazol-4-yl)amino]‑7H‑pyrrolo[2,3‑d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants

Journal of medicinal chemistry, 2016-03, Vol.59 (5), p.2005-2024

2016

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New Insights Regarding the Cyclization Pathway for Sterol Biosynthesis from (S)-2,3-Oxidosqualene

Journal of the American Chemical Society, 1995-11, Vol.117 (47), p.11819-11820

1995

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Discovery of potent and orally active MTP inhibitors as potential anti-obesity agents

Bioorganic & medicinal chemistry letters, 2006-06, Vol.16 (11), p.3039-3042

2006

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In vitro and in vivo profile of 2-(3-di-fluoromethyl-5-phenylpyrazol-1-yl)-5-methanesulfonylpyridine, a potent, selective, and orally active canine COX-2 inhibitor

Bioorganic & medicinal chemistry, 2005-03, Vol.13 (5), p.1805-1809

2005

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Structure-based design, SAR analysis and antitumor activity of PI3K/mTOR dual inhibitors from 4-methylpyridopyrimidinone series

Bioorganic & medicinal chemistry letters, 2013-05, Vol.23 (9), p.2787-2792

2013

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Abstract 3713: Identifying a mechanism of acquired resistance to the combined inhibition of PI3K/mTOR and MEK in colorectal carcinoma

Cancer research (Chicago, Ill.), 2014-10, Vol.74 (19_Supplement), p.3713-3713

2014

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Recent progress on third generation covalent EGFR inhibitors

Design and synthesis of a novel pyrrolidinyl pyrido pyrimidinone derivative as a potent inhibitor of PI3Kα and mTOR

Precedence and Promise of Covalent Inhibitors of EGFR and KRAS for Patients with Non-Small-Cell Lung Cancer

The development and SAR of pyrrolidine carboxamide 11β-HSD1 inhibitors

Quinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors

Targeting the mTOR pathway in tumor malignancy

4-Methylpteridinones as orally active and selective PI3K/mTOR dual inhibitors

The pharmacologic and toxicologic characterization of the potent and selective KRAS G12D inhibitors ERAS-4693 and ERAS-5024

5-Heteroatom substituted pyrazoles as canine COX-2 inhibitors. Part III: Molecular modeling studies on binding contribution of 1-(5-methylsulfonyl)pyrid-2-yl and 4-nitrile

5-Heteroatom substituted pyrazoles as canine COX-2 inhibitors. Part 1: Structure–activity relationship studies of 5-alkylamino pyrazoles and discovery of a potent, selective, and orally active analog

Comparative structure–activity relationship studies of 1-(5-methylsulfonylpyrid-2-yl)-5-alkyl and (hetero)aryl triazoles and pyrazoles in canine COX inhibition

Synthesis and SAR of heteroaryl-phenyl-substituted pyrazole derivatives as highly selective and potent canine COX-2 inhibitors

PF-04691502, a potent and selective oral inhibitor of PI3K and mTOR kinases with antitumor activity

5-Heteroatom-substituted pyrazoles as canine COX-2 inhibitors: Part 2. Structure–activity relationship studies of 5-alkylethers and 5-thioethers

Structure-Based Design and Synthesis of Potent and Selective KRAS G12D Inhibitors

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

Discovery of 1‑{(3R,4R)‑3-[({5-Chloro-2-[(1-methyl‑1H‑pyrazol-4-yl)amino]‑7H‑pyrrolo[2,3‑d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants

New Insights Regarding the Cyclization Pathway for Sterol Biosynthesis from (S)-2,3-Oxidosqualene

Discovery of potent and orally active MTP inhibitors as potential anti-obesity agents

In vitro and in vivo profile of 2-(3-di-fluoromethyl-5-phenylpyrazol-1-yl)-5-methanesulfonylpyridine, a potent, selective, and orally active canine COX-2 inhibitor

Structure-based design, SAR analysis and antitumor activity of PI3K/mTOR dual inhibitors from 4-methylpyridopyrimidinone series

Abstract 3713: Identifying a mechanism of acquired resistance to the combined inhibition of PI3K/mTOR and MEK in colorectal carcinoma

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