Abstract
A series of novel quinolone derivatives (8a-j) were synthesized, and their anticancer activities were tested in human cancer cell lines, human lung carcinoma cell (A549), human promyelocytic leukemia cell (HL-60), and human cervical cancer cell (Hela). Compound 8i was found to be 5-times more potent in cell-killing activity for cell lines A549, HL-60, and Hela than the positive control irinotecan or cisplatin, with IC50 of 0.009, 0.008 and 0.010 µM, respectively. The docking study revealed that compound 8i might have strong interactions with the active site of DNA-topoisomerase I.
Keywords:
anticancer; molecular docking; quinolone derivative; synthesis.
MeSH terms
-
Antineoplastic Agents / chemical synthesis
-
Antineoplastic Agents / chemistry
-
Antineoplastic Agents / pharmacology*
-
Cell Line, Tumor
-
Cell Proliferation / drug effects
-
DNA Topoisomerases, Type I / metabolism*
-
Dose-Response Relationship, Drug
-
Drug Screening Assays, Antitumor
-
Humans
-
Molecular Docking Simulation*
-
Molecular Structure
-
Quinolones / chemical synthesis
-
Quinolones / chemistry
-
Quinolones / pharmacology*
-
Structure-Activity Relationship
-
Topoisomerase I Inhibitors / chemical synthesis
-
Topoisomerase I Inhibitors / chemistry
-
Topoisomerase I Inhibitors / pharmacology*
Substances
-
Antineoplastic Agents
-
Quinolones
-
Topoisomerase I Inhibitors
-
DNA Topoisomerases, Type I
-
TOP1 protein, human