Abstract
A series of caffeic acid amides D1-D17 bearing 2,3,4,5-tetrahydrobenzo-[b][1,4]dioxocine units has been synthesized and their biological activities evaluated for potential antiproliferative and EGFR inhibitory activity. Of all the compounds studied, compound D9 showed the most potent inhibitory activity (IC50 = 0.79 μM for HepG2 and IC50 = 0.36 μM for EGFR). The structures of compounds were confirmed by 1H-NMR, ESI-MS and elemental analysis. Among all, the structure of compound D9 ((E)-N-(4-ethoxyphenyl)-3-(2,3,4,5-tetrahydrobenzo[b][1,4]dioxocin-8-yl)acrylamide) was also determined by single-crystal X-ray diffraction analysis. Compound D9 was found to be a potential antitumor agent according to biological activity, molecular docking, apoptosis assay and inhibition of HepG2.
Highlights
Cancer is a major cause of death in the World
In order to study the antitumor activities of (E)-3-(2,3,4,5-tetrahydrobenzo[b][1,4]dioxocin-8yl)acrylic acid amides, compounds D1-D17 were synthesized from caffeic acid
A series of caffeic acid amides D1-D17 bearing 2,3,4,5-tetrahydrobenzo[b] [1,4] dioxocin moieties has been synthesized and their biological activities were evaluated for potential antiproliferative and EGFR inhibitory activity
Summary
Cancer is a major cause of death in the World. In the United States one in four deaths is due to cancer [1]. Though we spend a lot of effort and money on research, control of advanced cancer has not Molecules 2014, 19 been achieved, so it is crucial to find novel cancer agents with new mode of action for saving lives. Many researchers have demonstrated that the EGFR can be seen as a rational target for anticancer [10,11]. Erlotinilb which could inhibit EGFR was approved as an antitumor agent a decade ago [12]
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