Synthesis and Biological Evaluation of Nitric Oxide-Donating Thalidomide Analogues as Anticancer Agents
Journal
Chemistry & Biodiversity
Journal Volume
6
Journal Issue
4
Pages
466-474
Date Issued
2009
Author(s)
Abstract
In search of more potent anticancer agents, 15 nitric oxide (NO)-donating thalidomide analogues, 6a, 6b, 8a-8e, and 13a-13h, were designed and synthesized. Cytotoxicity of these compounds was evaluated in vitro against three human tumor cell lines (HepG2, A549, and PC-3). The results indicated that 13a-13d exhibited notable anticancer activities comparable to or stronger than that of 5-fluorouracil (5-FU). Structure-activity relationships were also discussed, based on the experimental data obtained. Generally, the cytotoxic activity of target compounds is closely related to the type of NO donors, and the length of the spacers connecting to NO donors also appears important for the bioactivities.
SDGs
Type
journal article