A Building Block Approach for the Total Synthesis of YM-385781 |
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| Authors: | Dr. Yu Zhu Siyue Liu Johnny Zigmond Kevin M. Kaltenbronn Prof. Dr. Kendall J. Blumer Prof. Dr. Kevin D. Moeller |
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| Affiliation: | 1. Department of Chemistry, Washington University, St. Louis, MO-63130 USA;2. Department of Cell Biology and Physiology, Washington University School of Medicine, St. Louis, MO-63130 USA |
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| Abstract: | YM-254890 and FR900359 are potent and selective inhibitors of the Gq/11-signaling pathway. As such, they have been attractive targets for both synthesis and biological studies. Yet in spite of this effort, a versatile synthetic approach to the molecules that allows for the rapid construction of a variety of non-natural and labelled analogs and an increase in the amount of those analogs available remains elusive. We report here a convergent building block approach to the molecules that can solve this challenge. |
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| Keywords: | cyclic peptide synthesis inhibitors YM-analogs synthetic methods total synthesi |
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