In:
ChemMedChem, Wiley, Vol. 9, No. 5 ( 2014-05), p. 1030-1037
Abstract:
Cancer has been a primary global health issue for decades, with hepatocellular carcinoma (HCC) resulting in more than half a million new cases annually. With survival rates as low as 〈 5 % after five years, it remains a poorly treated cancer. Nordihydroguaiaretic acid (NDGA), an antioxidant, was previously proven effective against cancer cells. Nitroimidazole derivatives convert into reactive compounds under hypoxic conditions. In this study, eight methylated NDGAs containing a 2‐ or 4‐nitroimidazole moiety were synthesized as leads against HCC. Four of these conjugates, possessing a poly(ethylene glycol) tether, had superior aqueous solubility. These four NDGA–nitroimidazole conjugates were found to inhibit the proliferation HCC Hep3B cells with IC 50 values between 10 and 15 μ M . Furthermore, nitroimidazole‐conjugated NDGA derivatives exhibit better antiproliferative activity under hypoxic conditions.
Type of Medium:
Online Resource
ISSN:
1860-7179
,
1860-7187
DOI:
10.1002/cmdc.201300521
Language:
English
Publisher:
Wiley
Publication Date:
2014
detail.hit.zdb_id:
2209649-8
SSG:
15,3