Discovery and biological evaluation of potent dual ErbB-2/EGFR tyrosine kinase inhibitors: 6-thiazolylquinazolines
Discovery and biological evaluation of potent dual ErbB-2/EGFR tyrosine kinase inhibitors: 6-thiazolylquinazolines
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DOI：
10.1016/s0960-894x(02)01047-8
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发表时间：
2003-02-24
影响因子：
2.7
通讯作者：
Lackey, K
中科院分区：
文献类型：
--
作者：
Gaul, MD;Guo, Y;Lackey, K
我们已经确定了一类新的6-噻唑基喹唑啉作为ErbB-2和EGFR酪氨酸激酶活性的有效和选择性抑制剂，其IC50值在纳摩尔范围内。这些化合物在体外抑制过表达EGFR （HN5）和ErbB-2 （BT474）的人肿瘤细胞系的生长。使用同种细胞系的异种移植模型。我们发现，与对照动物相比，口服这些化合物可显著抑制体内肿瘤的生长。2003爱思唯尔科学有限公司版权所有。
We have identified a novel class of 6-thiazolylquinazolines as potent and selective inhibitors of both ErbB-2 and EGFR tyrosine kinase activity, with IC50 values in the nanomolar range. These compounds inhibited the growth of both EGFR (HN5) and ErbB-2 (BT474) over-expressing human tumor cell lines in vitro. Using xenograft models of the same cell lines. we found that the compounds given orally inhibited in vivo tumor growth significantly compared with control animals. (C) 2003 Elsevier Science Ltd. All rights reserved.