ADAM10 抑制剂 GI254023X 的改良合成。
Improved synthesis of ADAM10 inhibitor GI254023X.
机构信息
Clemens Schöpf Institute of Chemistry and Biochemistry, Technische Universität Darmstadt, Darmstadt, Germany.
出版信息
Neurodegener Dis. 2010;7(4):232-8. doi: 10.1159/000267865. Epub 2010 Feb 27.
BACKGROUND
The metalloproteinases ADAM10 and ADAM17 are involved in various diseases: neurodegeneration, cancer and inflammation.
OBJECTIVE
The inhibition of these proteases is a promising target in the treatment of inflammation and cancer.
METHODS AND RESULTS
In this study, we present an improved synthesis of the ADAM10 reference inhibitor GI254023X with a higher overall yield, enhanced detection ability and increased acid stability, providing easier handling.
CONCLUSION
This upscaled synthesis, free of diastereomeric intermediates, ensures single-batch identity, thus warranting its reproducibility in further biological investigations.
背景
金属蛋白酶 ADAM10 和 ADAM17 参与多种疾病：神经退行性疾病、癌症和炎症。
目的
抑制这些蛋白酶是治疗炎症和癌症的一个有前途的靶点。
方法和结果
在这项研究中，我们提出了一种改进的 ADAM10 参比抑制剂 GI254023X 的合成方法，该方法具有更高的总产率、增强的检测能力和增加的酸稳定性，便于操作。
结论
这种规模化合成方法不使用非对映异构体中间体，确保了单批物质的同一性，从而保证了其在进一步的生物学研究中的重现性。
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