Atropisomerism in the Pharmaceutically Relevant Realm

Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP-Deleted Cancers

(2022) Christopher R. Smith et al.   JOURNAL OF MEDICINAL CHEMISTRY

Development of Polar Organic Mode Chromatographic Method by Polysaccharide-Based Immobilized Chiral Selector and Validation for the Determination of the Enantiopurity of Novel Mineralocorticoid Receptor Antagonist Atropisomer–Esaxerenone

(2022) P. Radhakrishnanand et al.   CHROMATOGRAPHIA

Approaches toward Atropisomerically Stable and Conformationally Pure Diarylamines

(2022) Sagar D. Vaidya et al.   JOURNAL OF ORGANIC CHEMISTRY

Discovery and Optimization of 2H-1λ2-Pyridin-2-one Inhibitors of Mutant Isocitrate Dehydrogenase 1 for the Treatment of Cancer

(2021) Jason M. Rohde et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a Potent and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase with Oral Anti-Inflammatory Activity

(2021) Mark S. Tichenor et al.   ACS Medicinal Chemistry Letters

Emerging Approaches to Overcome Acquired Drug Resistance Obstacles to Osimertinib in Non-Small-Cell Lung Cancer

(2021) Matin Shaikh et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-Based Design and Pharmacokinetic Optimization of Covalent Allosteric Inhibitors of the Mutant GTPase KRASG12C

(2020) Jason G. Kettle et al.   JOURNAL OF MEDICINAL CHEMISTRY

Catalytic Atroposelective Synthesis of N-Aryl Quinoid Compounds

(2020) Sagar D. Vaidya et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Enantioselective Synthesis of N–C Axially Chiral Compounds by Cu‐Catalyzed Atroposelective Aryl Amination

(2020) Johanna Frey et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Close Amide NH···F Hydrogen Bonding Interactions in 1,8-Disubstituted Naphthalenes

(2020) Muhammad Kazim et al.   JOURNAL OF ORGANIC CHEMISTRY

Discovery of an Atropisomeric PI3Kβ Selective Inhibitor through Optimization of the Hinge Binding Motif

(2020) Stephane Perreault et al.   ACS Medicinal Chemistry Letters

Atropisomerism in diarylamines: structural requirements and mechanisms of conformational interconversion

(2020) Romain Costil et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Efficacy and safety of esaxerenone (CS-3150), a newly available nonsteroidal mineralocorticoid receptor blocker, in hypertensive patients with primary aldosteronism

(2020) Fumitoshi Satoh et al.   HYPERTENSION RESEARCH

Troponoid Atropisomerism: Studies on the Configurational Stability of Tropone-Amide Chiral Axes

(2019) Danielle R. Hirsch et al.   ORGANIC LETTERS

Structure-Guided Discovery of a Selective Mcl-1 Inhibitor with Cellular Activity

(2019) Zoltan Szlávik et al.   JOURNAL OF MEDICINAL CHEMISTRY

Leveraging Atropisomerism to Obtain a Selective Inhibitor of RET Kinase with Secondary Activities toward EGFR Mutants

(2019) Sean T. Toenjes et al.   ACS Chemical Biology

Structure-Based and Property-Driven Optimization of N-Aryl Imidazoles toward Potent and Selective Oral RORγt Inhibitors

(2019) Klemens Hoegenauer et al.   JOURNAL OF MEDICINAL CHEMISTRY

The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity

(2019) Jude Canon et al.   NATURE

Organocatalytic atroposelective construction of axially chiral arylquinones

(2019) Shuai Zhu et al.   Nature Communications

Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors

(2019) Brian A. Lanman et al.   JOURNAL OF MEDICINAL CHEMISTRY

Construction of Axially Chiral Compounds via Asymmetric Organocatalysis

(2018) Yong-Bin Wang et al.   ACCOUNTS OF CHEMICAL RESEARCH

Atropisomerism in medicinal chemistry: challenges and opportunities

(2018) Sean T Toenjes et al.   Future Medicinal Chemistry

Atropisomerism by Design: Discovery of a Selective and Stable Phosphoinositide 3-Kinase (PI3K) β Inhibitor

(2018) Jayaraman Chandrasekhar et al.   JOURNAL OF MEDICINAL CHEMISTRY

Enantioselective Synthesis of Pyrrolopyrimidine Scaffolds through Cation-Directed Nucleophilic Aromatic Substitution

(2018) Mariel M. Cardenas et al.   ORGANIC LETTERS

Atroposelective Catalytic Asymmetric Allylic Alkylation Reaction for Axially Chiral Anilides with Achiral Morita–Baylis–Hillman Carbonates

(2018) Shou-Lei Li et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Toward a Catalytic Atroposelective Synthesis of Diaryl Ethers Through C(sp2)–H Alkylation with Nitroalkanes

(2018) Jeffrey Gustafson et al.   SYNLETT

C797S Resistance: The Undruggable EGFR Mutation in Non-Small Cell Lung Cancer?

(2018) Tobias Grabe et al.   ACS Medicinal Chemistry Letters

Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia

(2018) Adriana E. Tron et al.   Nature Communications

Recent Progress of Small-Molecule Epidermal Growth Factor Receptor (EGFR) Inhibitors against C797S Resistance in Non-Small-Cell Lung Cancer

(2017) Lingfeng Chen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery and Assessment of Atropisomers of (±)-Lesinurad

(2017) Jianfei Wang et al.   ACS Medicinal Chemistry Letters

Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton’s Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers

(2016) Scott H. Watterson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Exploiting Atropisomerism to Increase the Target Selectivity of Kinase Inhibitors

(2015) Davis E. Smith et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Nonbiaryl and Heterobiaryl Atropisomers: Molecular Templates with Promise for Atropselective Chemical Transformations

(2015) Elango Kumarasamy et al.   CHEMICAL REVIEWS

Progress in Discovery of KIF5B-RET Kinase Inhibitors for the Treatment of Non-Small-Cell Lung Cancer

(2015) Minsoo Song   JOURNAL OF MEDICINAL CHEMISTRY

Analysis of Past and Present Synthetic Methodologies on Medicinal Chemistry: Where Have All the New Reactions Gone?

(2015) Dean G. Brown et al.   JOURNAL OF MEDICINAL CHEMISTRY

Atroposelective Synthesis of Axially Chiral Biaryldiols via Organocatalytic Arylation of 2-Naphthols

(2015) Ye-Hui Chen et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Enantioselective Synthesis of 3-Arylquinazolin-4(3H)-ones via Peptide-Catalyzed Atroposelective Bromination

(2015) Matthew E. Diener et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Organocatalytic Enantioselective Formal C(sp2)–H Alkylation

(2015) Madhu Sudan Manna et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Catalytic Enantioselective Synthesis of Atropisomeric Biaryls: A Cation-Directed Nucleophilic Aromatic Substitution Reaction

(2014) Roly J. Armstrong et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Mechanisms of RET signaling in cancer: Current and future implications for targeted therapy

(2014) I. Plaza-Menacho et al.   CELLULAR SIGNALLING

Inhibition of RET Increases the Efficacy of Antiestrogen and Is a Novel Treatment Strategy for Luminal Breast Cancer

(2014) P. M. Spanheimer et al.   CLINICAL CANCER RESEARCH

Analysis of the Structural Diversity, Substitution Patterns, and Frequency of Nitrogen Heterocycles among U.S. FDA Approved Pharmaceuticals

(2014) Edon Vitaku et al.   JOURNAL OF MEDICINAL CHEMISTRY

Profound Methyl Effects in Drug Discovery and a Call for New CH Methylation Reactions

(2013) Heike Schönherr et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Enantioselective Synthesis of Atropisomeric Benzamides through Peptide-Catalyzed Bromination

(2013) Kimberly T. Barrett et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Enantioselective Synthesis of Multisubstituted Biaryl Skeleton by Chiral Phosphoric Acid Catalyzed Desymmetrization/Kinetic Resolution Sequence

(2013) Keiji Mori et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Revealing Atropisomer Axial Chirality in Drug Discovery

(2011) Steven R. LaPlante et al.   ChemMedChem

Assessing Atropisomer Axial Chirality in Drug Discovery and Development

(2011) Steven R. LaPlante et al.   JOURNAL OF MEDICINAL CHEMISTRY

Biocatalytic Desymmetrization of an Atropisomer with both an Enantioselective Oxidase and Ketoreductases

(2010) Bo Yuan et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A novel therapeutic combination for neuroblastoma

(2010) Peter E. Zage et al.   CANCER

Insights into the Origins of Configurational Stability of Axially Chiral Biaryl Amines with an Intramolecular N−H−N Hydrogen Bond

(2010) Kazuhiro Hayashi et al.   JOURNAL OF ORGANIC CHEMISTRY

Enantioselective Synthesis of Biphenols from 1,4-Diketones by Traceless Central-to-Axial Chirality Exchange

(2010) Fenghai Guo et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Dynamic Kinetic Resolution of Biaryl Atropisomers via Peptide-Catalyzed Asymmetric Bromination

(2010) J. L. Gustafson et al.   SCIENCE

The Challenge of Atropisomerism in Drug Discovery

(2009) Jonathan Clayden et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Escape from Flatland: Increasing Saturation as an Approach to Improving Clinical Success

(2009) Frank Lovering et al.   JOURNAL OF MEDICINAL CHEMISTRY

Axially Chiral Binaphthyl Surrogates with an Inner N−H−N Hydrogen Bond

(2008) Takeo Kawabata et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A Randomized, Double-Blind, Phase IIa Dose-Finding Study of Vandetanib (ZD6474) in Japanese Patients With Non-Small Cell Lung Cancer

(2008) Katsuyuki Kiura et al.   Journal of Thoracic Oncology

Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells

(2008) L L Remsing Rix et al.   LEUKEMIA