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Design and synthesis of tricyclic cores for kinase inhibition |
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| Authors: | Stacy Van Epps Bryan Fiamengo Jeremy Edmunds Anna Ericsson Kristine Frank Michael Friedman Dawn George Jonathan George Eric Goedken Brian Kotecki Gloria Martinez Philip Merta Michael Morytko Shashank Shekhar Barbara Skinner Kent Stewart Jeffrey Voss Grier Wallace Neil Wishart |
| Affiliation: | 1. Abbott Bioresearch Center, 381 Plantation St, Worcester, MA 01605, USA;2. Abbott Laboratories, 100 Abbott Park Rd, Abbott Park, IL 60064, USA;3. Abbott Laboratories, 1401 Sheridan Rd, North Chicago, IL 60064, USA;4. Forma Therapeutics, 500 Arsenal St, Watertown, MA 02472, USA;5. Abbott Laboratories, 381 Plantation St. Worcester MA, USA |
| Abstract: | Interest in therapeutic kinase inhibitors continues to grow beyond success in oncology. To date, ATP-mimetic kinase inhibitors have focused primarily on monocyclic and bicyclic heterocyclic cores. We sought to expand on the repertoire of potential cores for kinase inhibition by exploring tricyclic variants of classical bicyclic hinge binding motifs such as pyrrolopyridine and pyrrolopyrazine. Herein we describe the syntheses of eight alternative tricyclic cores as well as in vitro screening results for representative kinases of potential therapeutic interest. |
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