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

  • Bioorg Med Chem Lett. 2016 May 1;26(9):2355-9. doi: 10.1016/j.bmcl.2016.03.012.
Chunlan Wang  1 ,  Guimin Xia  1 ,  Xiujun Liu  2 ,  Rui Zhang  1 ,  Yun Chai  1 ,  Jun Zhang  3 ,  Xiaoning Li  1 ,  Yang Yang  1 ,  Juxian Wang  1 ,  Mingliang Liu  4
Affiliations
  • 1. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
  • 2. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China. Electronic address: [email protected].
  • 3. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China; Zhejiang Starry Pharmaceutical Co. Ltd, Xianju 317300, China.
  • 4. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China. Electronic address: [email protected].
PMID: 26995527 DOI: 10.1016/j.bmcl.2016.03.012
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).

Keywords
ATB-429 derivatives; Antitumor activity; Nitric oxide; Synthesis.