JinJiang Zhu

Discovery of (10 <i>R</i> )-7-Amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro- <i>2H</i> -8,4-(metheno)pyrazolo[4,3- <i>h</i> ][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a Macrocyclic Inhibitor of Anaplastic Lymphoma Kinase (ALK) and c-ros Oncogene 1 (ROS1) with Preclinical Brain Exposure and Broad-Spectrum Potency against ALK-Resistant Mutations

Ted W. Johnson, Paul Richardson, Simon Bailey et al. · Journal of Medicinal Chemistry · 2014 · 585 citations · Full text

Medicine, Medicinal Chemistry, Pharmacology +16

Strain-release amination

Ryan Gianatassio, Justin M. Lopchuk, Jie Wang et al. · Science · 2016 · 580 citations

Pharmacy, Medicinal Chemistry, Bioisosterism +5

Strain-Release Heteroatom Functionalization: Development, Scope, and Stereospecificity

Justin M. Lopchuk, Kasper Fjelbye, Yu Kawamata et al. · Journal of the American Chemical Society · 2017 · 344 citations · Full text

Pharmacy, Medicinal Chemistry, Bioisosterism +14

Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (<i>R</i>)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2<i>H</i>)-one (PF-06821497)

Pei‐Pei Kung, Patrick Bingham, Alexei Brooun et al. · Journal of Medicinal Chemistry · 2017 · 128 citations · Full text

Pharmacy, Medicinal Chemistry, Pharmacology +17

Design of Potent and Selective Inhibitors to Overcome Clinical Anaplastic Lymphoma Kinase Mutations Resistant to Crizotinib

Qinhua Huang, Ted W. Johnson, Simon Bailey et al. · Journal of Medicinal Chemistry · 2014 · 118 citations · Full text

Medicine, Oncology, Pharmacology +14