A Building Block Approach for the Total Synthesis of YM-385781

Yu Zhu; Siyue Liu; Johnny Zigmond; Kevin M. Kaltenbronn; Kendall J. Blumer; Kevin D. Moeller

doi:10.1002/ejoc.202300365

A Building Block Approach for the Total Synthesis of YM-385781

Yu Zhu, Siyue Liu, Johnny Zigmond, Kevin M. Kaltenbronn, Kendall J. Blumer, Kevin D. Moeller

Research output: Contribution to journal › Article › peer-review

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.

Original language	English
Article number	e202300365
Journal	European Journal of Organic Chemistry
Volume	26
Issue number	20
DOIs	https://doi.org/10.1002/ejoc.202300365
State	Published - May 22 2023

Keywords

YM-analogs
cyclic peptide synthesis
inhibitors
synthetic methods
total synthesi

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10.1002/ejoc.202300365

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AU - Zigmond, Johnny

AU - Kaltenbronn, Kevin M.

AU - Blumer, Kendall J.

AU - Moeller, Kevin D.

PY - 2023/5/22

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AB - 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.

KW - YM-analogs

KW - cyclic peptide synthesis

KW - inhibitors

KW - synthetic methods

KW - total synthesi

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JO - European Journal of Organic Chemistry

JF - European Journal of Organic Chemistry

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A Building Block Approach for the Total Synthesis of YM-385781

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