期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 21, 期 11, 页码 3147-3153出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.03.033
关键词
Quinoline; Anilinoquinoline; DNMT1 inhibitor; Synthesis
资金
- Supergen Inc.
- Cancer Society Auckland
A series of 4-anilinoquinoline derivatives related to the known inhibitor SGI-1027, containing side chains of varying pK(a), were prepared by acid-catalysed coupling of the pre-formed side chains with 4-chloroquinolines. The compounds were evaluated for their ability to reduce the level of DNMT1 protein in HCT116 human colon carcinoma cells by Western blotting. With a very strongly basic N-methylpyridinium side chain, only NHCO-linked compounds were effective, whereas less strongly basic ((diaminomethylene) hydrazono)ethyl or 3-methylpyrimidine-2,4-diamine side chains allowed both NHCO- and CONH-linked compounds to show activity. In contrast, the pK(a) of the quinoline unit had little apparent influence on activity. (C) 2013 Elsevier Ltd. All rights reserved.
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