1.Synthesis and in vitro antitumor activities of novel benzyl urea analogues of sorafenib.
Chenshu LU ; Ke TANG ; Yan LI ; Bo JIN ; Dali YIN ; Chen MA ; Xiaoguang CHEN ; Haihong HUANG
Acta Pharmaceutica Sinica 2013;48(5):709-17
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.
Result Analysis
Print
Save
E-mail