Leveraging conformational control about a potential atropisomeric axis as a strategy in medical chemistry

Axially‐Chiral Cannabinols: A New Platform for Cannabinoid‐Inspired Drug Discovery

(2020) Alexander J. Grenning et al.   ChemMedChem

Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer

(2020) Jay B. Fell 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

Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors

(2019) Harald Engelhardt et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor

(2018) Matthew R. Janes et al.   CELL

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

Structural and Atropisomeric Factors Governing the Selectivity of Pyrimido-benzodiazipinones as Inhibitors of Kinases and Bromodomains

(2018) Jinhua Wang et al.   ACS Chemical Biology

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

First macrocyclic 3 rd -generation ALK inhibitor for treatment of ALK/ROS1 cancer: Clinical and designing strategy update of lorlatinib

(2017) Sulman Basit et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Conformational Studies and Atropisomerism Kinetics of the ALK Clinical Candidate Lorlatinib (PF-06463922) and Desmethyl Congeners

(2016) Jeff Elleraas et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Exploiting Atropisomerism to Increase the Target Selectivity of Kinase Inhibitors

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

Assessing Atropisomer Axial Chirality in Drug Discovery and Development

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

The Medicinal Chemist’s Toolbox: An Analysis of Reactions Used in the Pursuit of Drug Candidates

(2011) Stephen D. Roughley et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

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