Synthesis and biomedicinal investigation of novel styryl lactone and antitumor agent tiazofurin bioisosteres

U ovom radu prikazana je sinteza 11 tiazolnih izostera goniofufurona (1-11), 4 konformaciono kruta analoga goniofufurona (12-15) i jednog butadiolnog derivata tiazofurina (16). Takođe, izvršeno je ispitivanje i poređenje bioloških aktivnosti sintetisanih analoga sa sa aktivnošću i selektivnošću kako GF i TF tako i doksorubicina, jedinjenja širokog spektra dejstva (DOX). Hiralni prekursor novosintetisanih jedinjenja 1-15 bila je D-glukoza, a jedinjenja 16 D-arabinoza.A multistep synthesis of 11 novel thiazole isosteres of goniofufurone (1-11), 4 novel conformationally constrained isosteres of goniofufurone (12-15), as well as one butanediole derivative of tiazofurin (16) has been achieved. In vitro cytotoxicity of newly synthetized derivatives has been evaluated and compared with the cytotoxicities of goniofufurone, tiazofurin and doxorubicin