Abstract
A series of squaramates and squaramides have been synthesized and their cytotoxic activity has been investigated in different cancer cell lines.
Highlights
The field of squaramides has experienced an extraordinary growth since the work reported by Rawal and co-workers in 2008,1 where these molecules were used as organocatalysts
Cell-type specific cytotoxic effect of squaramides The effect of squaramides on cell viability was initially evaluated on different tumor cell lines (HeLa, cervical carcinoma, and HGC-27, gastric carcinoma) using an MTT assay after 24 h of treatment at 100 μM (Fig. 1)
It has been shown that substituted squaramide 34 effectively inhibited the proliferation of HGC-27 cells in a concentration-dependent manner
Summary
The field of squaramides has experienced an extraordinary growth since the work reported by Rawal and co-workers in 2008,1 where these molecules were used as organocatalysts. In spite of the increasing number of bioactive squaramidebased compounds found in the literature, their application as anticancer agents has not yet been intensively explored and no exhaustive studies in different cancer cells have been previously reported.[17,18] In addition, some squaramides have been shown to selectively bind protein kinases[18] or the CXCR2 receptor,[19] indicating that this class of compounds may exert their function by selectively binding to cellular targets. This, together with the interest in searching for new anticancer agents, prompted us to evaluate the antitumor activity of a variety of squaramides synthesized following a protocol recently published by us.[20,21,22]
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