4-Substituted-2-phenylquinazolines as inhibitors of BCRP
摘要:
We investigated several 2-phenylquinazolines with different substitutions at position 4 for their BCRP inhibition. Compounds with phenyl ring attached via an amine-containing linker at position 4 were found to be potent inhibitors of BCRP. In general compounds with meta substitution of phenyl ring at position 4 were found to have higher inhibitory effect, compound 12 being the most potent and selective towards BCRP. (C) 2012 Elsevier Ltd. All rights reserved.
Synthesis, analgesic and anti-inflammatory evaluation of some novel quinazoline derivatives
作者:Ahmed M. Alafeefy、Adnan A. Kadi、Omar A. Al-Deeb、Kamal E.H. El-Tahir、Nabila A. Al-jaber
DOI:10.1016/j.ejmech.2010.07.067
日期:2010.11
Two series of somenew 2,4,6-trisubstituted-quinazoline derivatives were prepared and screened for their analgesic, anti-inflammatory activity and acute toxicity. Four compounds were more potent analgesic agents than the reference drug Indomethacin and thirteen compounds showed significant anti-inflammatory activity. Seven compounds showed combined ability to inhibit both pain and inflammation. Compounds