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Updated: Jul 7, 2025

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基于Pyrazole的宏循环的合成导致MST3的高度选择性抑制剂

Jennifer Alisa Amrhein1,2, Lena Marie Berger1,2, Dimitrios-Ilias Balourdas1,2

  • 1Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.

Journal of medicinal chemistry
|December 21, 2023
PubMed
概括

研究人员开发了JA310,这是第一个选择性化学探针,用于哺乳动物无菌20样氨酸/氨酸激酶3 (MST3). 这种抑制剂显示出高强度和选择性,有助于MST3.

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α-Substituted ketones or aldehydes can be synthesized from enamines by the Stork enamine reaction, named after its pioneer Gilbert Stork. Enamines are useful synthetic intermediates where the lone pair on nitrogen is in conjugation with the C=C bond. They resemble enolate ions, as the resonance forms of both species have a nucleophilic α carbon.
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