Synthesis and in vitro antitumor activities of novel benzyl urea analogues of sorafenib / 药学学报
Acta Pharmaceutica Sinica
;
(12): 709-717, 2013.
Article
in English
| WPRIM
| ID: wpr-235606
ABSTRACT
A novel series of benzyl urea analogues based on the structural modification of sorafenib were synthesized. Their in vitro antitumor activities against MX-1, HepG2, Ketr3 and HT-29 were evaluated using the standard MTT assay. While several target compounds showed inhibitory activity against multiple cancer cell lines, compound 9 was of particular interest, demonstrating IC50 values (5.69-13.6 micromol x L(-1)) comparable to those of sorafenib. Furthermore, compounds 20 and 23 showed more potent inhibitory activity against HT-29 and MX-1 when compared to sorafenib. In particular, compound 20 bearing the N-3-pyridyl moiety not only exhibited greater inhibitory activity against HT-29 cell line (IC50 3.82 micromol x L(-1)), but also had improved solubility at pH 7.2, is worthy of further investigation as a lead to identify novel antitumor agents.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pharmacology
/
Phenylurea Compounds
/
Solubility
/
Structure-Activity Relationship
/
Urea
/
Drug Screening Assays, Antitumor
/
Molecular Structure
/
Chemistry
/
Niacinamide
/
HT29 Cells
Limits:
Humans
Language:
English
Journal:
Acta Pharmaceutica Sinica
Year:
2013
Type:
Article
Similar
MEDLINE
...
LILACS
LIS