engleski

Synthesis, photochemical synthesis and antitumor evaluation in vitro of novel derivatives of benzothieno and thienothieno quinolones

Heterocyclic amides and their cyclic derivatives, quinolones, are structural part of a large number of natural compounds. Due to the wide range of biological activities, they are the subject of intense research of synthetic organic and medicinal chemists with the aim of finding selective therapeutic agents.1 Previously prepared derivatives of benzo[b]thieno-, thieno[2', 3':4, 5]thieno- and thieno[3', 2':4, 5]thieno[2, 3-c]quinolones showed very good antitumor activity in vitro on a number of human tumor cell lines. Some of these compounds efficiently bind to double- stranded polynucleotides by intercalation.2, 3 Searching for compounds related to these classes of biologically and pharmacologically active compounds, new derivatives of benzo[b]thiophene, thieno[2, 3-b]thiophene and thieno[3, 2-b]thiophene carboxamides were prepared in a multistep synthesis.4 Their cyclic analoges were prepared by photochemical dehydrohalogenation. All compounds were characterized by 1H, 13C NMR, IR and UV/Vis spectroscopy. Antitumor activity in vitro was tested on 5 human tumor cell lines. Based on in vitro screening results all compounds showed high antiproliferative effect.

Synthesis; photochemical synthesis and antitumor evaluation in vitro; benzothieno and thienothieno quinolones

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