Cyclopeptide compound containing epoxy ketone as well as preparation method and application of cyclopeptide compound
The invention provides a cyclopeptide compound containing epoxy ketone as well as a preparation method and application of the cyclopeptide compound. Specifically, the invention provides a compound as shown in a formula I, # imgabs0 # cyclopeptide compound as shown in the formula I, cysteine and lysi...
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Format: | Patent |
Sprache: | chi ; eng |
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Zusammenfassung: | The invention provides a cyclopeptide compound containing epoxy ketone as well as a preparation method and application of the cyclopeptide compound. Specifically, the invention provides a compound as shown in a formula I, # imgabs0 # cyclopeptide compound as shown in the formula I, cysteine and lysine side chains in linear peptide are cyclized with phthalic dicarboxaldehyde, and then the cyclized product and epoxy ketone fragments are condensed to obtain the compound. The cyclopeptide epoxy ketone compound disclosed by the invention has good proteasome inhibition activity and shows a relatively good inhibition effect on hematoma and solid tumor cell strains.
本发明提供了一种含环氧酮的环肽化合物、其制备方法及应用。具体地,本发明提供了式I所示的化合物,#imgabs0#式I所述环肽化合物,通过线性肽中半胱氨酸、赖氨酸侧链,与邻苯二甲醛环合,再与环氧酮片段缩合得到。本发明的环肽环氧酮类化合物具有良好的蛋白酶体抑制活性,在血液瘤和实体瘤细胞株上均展现了较好的抑制作用。 |
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