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Synthesis, Antitumor Activity and QSAR Analysis of Heterocyclic Amides and Quinolones

The development of effective antineoplastic drugs has become one of the most intensively studied aspect of contemporary medicinal chemistry and therefore has been tremendous growth in the number and types of new anticancer agents. Substituted heterocyclic amides and their fused analogues quinolones showed wide range of biological activity and are still intensively investigated. We have previously reported synthesis and strong inhibitory activities on several human cell lines of various amidino substituted benzobthiophene-2-carboxamides and benzo[b]thieno[2, 3-c]quionolones. In this report we are presenting synthesis, antiproliferative activity and QSAR analysis of some novel thiophene-2-carboxamides and their fused analogues quinolones as a part of our continuing research of polyfunctional heterocyclic compounds. For the synthesis of novel compounds were used both classic methods of organic synthesis as well as photochemical procedures. Prepared compounds were tested on their antitumor activity on several human tumour cell lines. Using measurements of antitumor activity of heterocyclic amides and quinolones 3D–Quantitative Structure–Activity Relationship (3D-QSAR) models were built. Volsurf based procedure, which is independent of the alignment of molecules, was used. Using this knowledge, new compounds were proposed for synthesis and biological testing. Their activities were predicted using the derived QSAR models and the proposed compounds were shown as promising antitumor candidates.

thiophene-2-carboxamides ; antitumor activity ; 3D–Quantitative Structure Activity Relationship

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