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作为Raf-1抑制剂的苯并噻唑酰胺和脲衍生物的合成

Synthesis of amide and urea derivatives of benzothiazole as Raf-1 inhibitor.

作者信息

Song Eun Young, Kaur Navneet, Park Mi-Young, Jin Yinglan, Lee Kyeong, Kim Guncheol, Lee Ki Youn, Yang Jee Sun, Shin Jae Hong, Nam Ky-Youb, No Kyoung Tai, Han Gyoonhee

机构信息

Korea Research Institute of Bioscience and Biotechnology (KRIBB), Yuseong-Gu, Daejeon, Republic of Korea.

出版信息

Eur J Med Chem. 2008 Jul;43(7):1519-24. doi: 10.1016/j.ejmech.2007.10.008. Epub 2007 Oct 11.

DOI:10.1016/j.ejmech.2007.10.008
PMID:18023932
Abstract

A series of amide and urea derivatives of benzothiazole have been synthesized and evaluated for their antiproliferative profile in human SK-Hep-1 (liver), MDA-MB-231 (breast), and NUGC-3 (gastric) cell lines. Among them, compounds 1-2, 16-18, 23, and 25-26 had potent to moderate inhibitory activities. Further these compounds were investigated for their ability to inhibit Raf-1 activity.

摘要

已经合成了一系列苯并噻唑的酰胺和脲衍生物，并在人SK-Hep-1（肝脏）、MDA-MB-231（乳腺）和NUGC-3（胃）细胞系中评估了它们的抗增殖特性。其中，化合物1-2、16-18、23和25-26具有强效至中等强度的抑制活性。此外，还研究了这些化合物抑制Raf-1活性的能力。

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