Quinoline derivatives as anti-cancer agents

摘要

Quinoline derivatives showing anticancer activities against cancer cell lines of hepatocellular carcinoma (Hep3B), lung carcinoma (A549), esophageal squamous cell carcinoma (HKESC-1, HKESC-4 and KYSE150). The quinoline derivatives have a backbone structure of the following formulas:;

主权项

1. A quinoline derivative, comprising a structure of the following formula: wherein R1 and R3 are independently of each other H or Br; wherein each of R2, R7 and R8 is H; wherein R4 is CN, 2-(piperdin-1-yl)ethoxy, biphenyl-3-ylmethoxy, OH, OAc, or OR′, wherein R′ is a phenyl group having the following formula: wherein Ra is CH2 or SO2; Rb and Rc independently are H, Cl, F, OCH3, CH3, Ph, NO2, CF3 or OCF3; wherein R5 is H or COCH3; wherein R6 is CH3, OH, CH2OH, CH2CH2Ph, CH2CH3, OBn, COOH, CHO, 3,4-dimethoxyphenethyl or a phenyl group having the following formula: wherein Ra is CH2NH; Rb and Rc independently of each other are H, C(CH3)3, OCH3, OPh, COH2Ph or morpholinyl;
provided that when R2, R5, R7 and R8 are H, and R4 is OH, then R6 is not CH3;provided that when R1, R2, R3, R7 and R8 are H, R6 is CH3, and R4 is an alkoxy, then R5 is not H; andprovided that when R1 is Br, R2, R3, R5, R7 and R8 are H, and R6 is CH3, then R4 is not OH;and salts thereof.