期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 12, 页码 3526-3529出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.04.139
关键词
PI3K inhibitor; mTOR inhibitor
A series of 5-ureidobenzofuran-3-one indoles as potent inhibitors of PI3K alpha and mTOR has been developed. The best potency in cells was obtained when the urea group was extended to a 4-[2-(dimethylamino)ethyl]methylamino amidophenyl group. A 7-fluoro group on the indole ring also enhanced cellular potency. Compound 18i, incorporating the optimal functional groups, showed high potency in cellular lines and was further studied in vivo. It was able to inhibit the biomarker phosphorylation for 8 h when dosed at 25 mg/kg iv. In the MDA-MB-361 breast cancer model, it shrank the tumor size remarkably when dosed at 25 mg/kg iv on days 1, 5, and 9. (C) 2010 Elsevier Ltd. All rights reserved.
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