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Comparison of antitumor activity of some benzothiophene, thienothiophene, carboxanilides and quinolones in 2D and 3D cell culture system

One of the main reasons of high drug attrition rate in oncology is poor clinical predictive power of 2D cell cultures that are historically used as a standard tool for in vitro assays as an integral part of drug discovery process. For this reason, there is increasing interest in developing 3D in vitro cell culture systems which represent a biologically relevant assay system, feasible for the development of robust preclinical anti-cancer drug screening platforms. Over the past few years substituted heterocyclic derivatives have been one of the most extensively studied classes of organic compounds due to their well known biological activities. Substituted heterocyclic quinolones and carboxamides exhibit several pharmacological activities and have therefore attracted considerable attention from medicinal and synthetic organic chemists. As a part of our continuing search for potential anticancer agents related to heterocyclic quinolones, we have previously reported synthesis and strong inhibitory activities on several human tumour cell lines of versatile benzothiophene and thienothiophene carboxanilides and quinolones (Fig. 1) thus confirming the anticancer potential of this class of compounds [1]. In addition, 3D hanging-drop cell culture method was applied on a human cancer breast cell lines (SK-BR-3, MDA-MB-231, T-47D) and their antitumor activity in vitro ion 2D cell culture was compared with activity of 3D cell culture system. Obtained results in some cases showed significant disagreement indicating that some prominent compounds can be discarded in early phase of researching while chance was given to compounds with false positive result.

antitumor activity; benzothiophenes; carboxanilides; thienothiophenes; quinolones; 2D and 3D in vitro assay

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