Synthesis and biological evaluation of 2-(3-butynoicamidophenyl) benzothiazole derivatives as antitumor agents / 药学学报
Acta Pharmaceutica Sinica
;
(12): 888-895, 2014.
Article
in Chinese
| WPRIM
| ID: wpr-244998
ABSTRACT
A series of 2-(3-butynoicamidophenyl)benzothiazole derivatives were synthesized starting from 4-fluoro-3-nitrobenzoic acid. Structures of all the synthesized compounds were confirmed by 1H NMR and HR-MS. Their antitumor activities against human tumor cells lines (HCT116, Mia-PaCa2, U87-MG, A549, NCI-H1975) were evaluated by MTT assay. The results revealed that most of the synthesized compounds showed potent activities against HCT116, Mia-PaCa2, U87-MG tumor cells lines. Particularly, compounds 14c and 14h exhibited better activity with IC50 values of 1 x 10(-8) mol x L(-1) against U87-MG and HCT116 respectively. The structure-activity relationship of compounds was also discussed preliminarily.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pharmacology
/
Structure-Activity Relationship
/
Drug Screening Assays, Antitumor
/
Cell Line, Tumor
/
Benzothiazoles
/
Antineoplastic Agents
/
Nitrobenzoates
Limits:
Humans
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2014
Type:
Article
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