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Synthesis and antitumor evaluation of a novel series of triaminotriazine derivatives.

Abstract：

:A series of triaminotriazine derivatives (compounds 5a-f, 6a-x, and 7a-g) was designed, synthesized, and evaluated for their inhibition activities to colorectal cancer (CRC) cell lines (HCT-116 and HT-29). Most of the synthesized compounds demonstrated moderate anti-proliferatory effects on both HCT-116 and HT-29 cell lines at the concentration of 10 microM. The inhibitory activities against HCT-116 and HT-29 cell lines were discussed to develop the structure-activity relationships of this new series. Compounds 6l and 6o exhibited prominent inhibition activities toward HCT-116, with IC50s of 0.76 and 0.92 microM, respectively. The in vivo antitumor studies and pharmacokinetics of compound 6l showed that it might be a promising new hit for further development of antitumor agents.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Zheng M,Xu C,Ma J,Sun Y,Du F,Liu H,Lin L,Li C,Ding J,Chen K,Jiang H

doi

10.1016/j.bmc.2006.11.028

subject

Has Abstract

pub_date

2007-02-15 00:00:00

pages

1815-27

issue

4

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(06)00956-4

journal_volume

15

pub_type

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