In vitro cytotoxicity of benzopyranone derivatives with basic side chain against human lung cell lines.
BACKGROUND
Coumarins belong to an important group of useful drugs with diverse pharmacological properties. In the present study, the in vitro cytotoxicity of new coumarin-based benzopyranone derivatives containing diethylaminoethoxy (5), dimethylaminoethoxy (6), morpholinoethoxy (7), piperidinylethoxy (8) and pyrrolidinylethoxyl (9) amino side chain against human carcinoma (A549) and normal (LL47) lung cell lines was evaluated.


METHODS
The cytotoxicity was evaluated by crystal violet dye binding assay. The effect of compound 9 on different phases of the cell cycle was determined using flow cytometry.


RESULTS
In A549 cells, the 50% lethal dose (LD(50)) for compounds 5-9 were found to be 7.08, 5.0, 34.2, 8.33 and 5.83 μM, respectively, while in LL47 cells, the LD(50) values were found to be 16.7, 20.4, 34.6, 15.4 and 8.75 μM, respectively after 48 h treatment. Cell cycle data indicated that A549 cells were arrested at different phases depending on the concentration.


CONCLUSIONS
Compounds 5-9 showed anticancer activity against lung cancer cell lines, while compound 6 showed highly selective anticancer activity.
Departments of 1Chemistry and 2Biology, Florida A and M University, Tallahassee, FL 32307 32307, USA. musiliyu.musa@famu.edu
Musiliyu A
MA
Musa
Veera L D
VL
Badisa
Lekan M
LM
Latinwo
Caroline
C
Waryoba
Ngozi
N
Ugochukwu
D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D002470:Cell Survival; D002478:Cells, Cultured; D003374:Coumarins / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D005434:Flow Cytometry; D006801:Humans; D066298:In Vitro Techniques; D008168:Lung / Q000187:drug effects; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000473:pathology*
D003374:Coumarins