Hollis Showalter joined the University of Michigan in 2006 after more than 25 years of drug discovery and development experience within the pharmaceutical industry. He has broad experience in synthetic medicinal chemistry and has contributed to a number of campaigns resulting in agents proceeding to clinical trials. One of these, Nipent™, is marketed for the treatment of hairy cell leukemia. He was the founding Director of the University of Michigan Vahlteich Medicinal Chemistry Core (UMVMCC.org), which works with collaborators in hit-to-lead campaigns to advance their drug discovery efforts, contribute synthetic and medicinal chemistry strategies to grant proposals, and develop biological probes or potential therapeutic agents for biological investigation. He also provides expertise on intellectual property protection. He has published 167 peer reviewed manuscripts/reviews/book chapters, and 157 meeting abstracts. He holds 46 issued or applied for patents.
He has served professionally on numerous internal and external committees, including industry, UM, and the American Chemical Society Medicinal Chemistry Division.
For a complete profile of Showalter’s professional history, refer to his CV.
Natural products modification and heterocyclic chemistry synthesis
Designing in physicochemical properties to high-throughput screen hits that confer “druggability” (e.g., conformity to Lipinski rules, absence of toxicophores)
Development of structure-activity relationships (SAR) to derive compounds with optimal pharmacokinetic and metabolic profiles toward the initiation of in vivo studies
Principal therapeutic focus in bacterial diseases and oncology with extensive knowledge of associated targets, e.g., RNA polymerase and protein kinases
Gan X, Showalter HD, A Concise Synthesis of 3-Substituted-7-Amino-6-Carboxyl-8-Azachromones, Tet. Lett., 2019, 60: 2035 - 2037.
McDonald AJ, Leon DR, Markham KA, Wu B, Heckendorf CF, Schilling K, Showalter HD, Andrews PC, McComb ME, Pushie MJ, Costello CE, Millhauser GL, Harris DA. Altered Domain Structure of the Prion Protein Caused by Cu2+ Binding and Functionally Relevant Mutations: Analysis by Cross-Linking, MS/MS, and NMR. Structure, 2019, 27: 907-922.e5. PMID: 30956132.
Beyett TS, Gan X, Reilly SM, Gomez AV, Chang L, Tesmer JJG, Saltiel AR, Showalter HD. Design, Synthesis and Biological Activity of Substituted 2-Amino-5-oxo-5H-chromeno[2,3-b]pyridine-3-carboxylic Acid Derivatives as Inhibitors of the Inflammatory Kinases TBK1 and IKK for the Treatment of Obesity. Bioorg. Med. Chem., 2018, 26: 5443-5461. PMID: 30270002.
Madak JT, Cuthbertson CR, Miyata Y, Tamura S, Petrunak EM, Stuckey JA, Han Y, He M, Sun D, Showalter HD, Neamati N. Design, Synthesis, and Biological Evaluation of 4-Quinoline Carboxylic Acids as Inhibitors of Dihydroorotate Dehydrogenase. J. Med. Chem., 2018, 61: 5162–5186. PMID: 29727569.