Kristin Goldberg

Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia

Melissa B. Pappalardi, Kathryn Keenan, Mark Cockerill et al. · Nature Cancer · 2021 · 280 citations · Full text

Medicine, Oncology, Pharmacology +8

Use of Small-Molecule Crystal Structures To Address Solubility in a Novel Series of G Protein Coupled Receptor 119 Agonists: Optimization of a Lead and in Vivo Evaluation

James S. Scott, Alan M. Birch, Katy J. Brocklehurst et al. · Journal of Medicinal Chemistry · 2012 · 75 citations · Full text

Pharmacy, Medicinal Chemistry, Pharmacology +17

Discovery of <i>N</i>-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1<i>H</i>-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors

Jason G. Kettle, Rana Anjum, Evan Barry et al. · Journal of Medicinal Chemistry · 2018 · 62 citations · Full text

Pharmacy, Medicinal Chemistry, Pharmacology +14

Oxadiazole isomers: all bioisosteres are not created equal

Kristin Goldberg, Sam D. Groombridge, Julian A. Hudson et al. · MedChemComm · 2012 · 44 citations

Pharmacy, Chemistry, Medicinal Chemistry +16

The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity

Rebecca Newton, Katherine A. Bowler, Emily M. Burns et al. · European Journal of Medicinal Chemistry · 2016 · 39 citations · Full text

Pharmacy, Medicinal Chemistry, Pharmacology +13