Journal
MOLECULES
Volume 17, Issue 5, Pages 5870-5881Publisher
MDPI AG
DOI: 10.3390/molecules17055870
Keywords
2-substituted-4-amino-6-halogenquinolines; design; synthesis; antiproliferative activity
Funding
- National S & T Major Project [2011ZX09102-001-006]
- S & T Project of Liaoning Province [LJQ201107]
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Two series of novel 2-substituted-4-amino-6-halogenquinolines 8a-l and 13a-h were designed, synthesized and evaluated for their antiproliferative activity against H-460, HT-29, HepG2 and SGC-7901 cancer cell lines in vitro. The pharmacological results indicated that most compounds with 2-arylvinyl substituents exhibited good to excellent antiproliferative activity. Among them, compound 8e was a considered promising lead for further structural modifications with IC50 values of 0.03 mu M, 0.55 mu M, 0.33 mu M and 1.24 mu M, which was 2.5- to 186-fold more active than gefitinib and compound 1.
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