Synthesis and antitumor activity of ATB-429 derivatives containing a nitric oxide-releasing moiety.

ABSTRACT

A series of novel ATB-429 (an anti-inflammatory candidate) derivatives containing a nitric oxide (NO)-releasing moiety were designed, synthesized and evaluated for their in vitro activity against six human cancer cell lines. Our results reveal that phenylsulfonylfuroxan-based derivatives have considerable antitumor activity, and compounds 7-9 (IC50s 0.256-3.024 µM) against HT-29 and PANC-1, 8a,b (IC50s 2.677-3.051 µM) against MCF-7 and 8a (IC50 1.270 µM) against DU145 are more active than Vandetanib (IC50s 1.925-4.107 µM).