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Sinteza i biomedicinska ispitivanja novih bioizostera stiril-laktona i antitumorskog agensa tiazofurina / Synthesis and biomedicinal investigation of novel styryl lactone and antitumor agent tiazofurin bioisosteresSvirčev Miloš 26 September 2018 (has links)
<p>U ovom radu prikazana je sinteza 11 tiazolnih izostera goniofufurona (1-11),<br />4 konformaciono kruta analoga goniofufurona (12-15) i jednog butadiolnog<br />derivata tiazofurina (16). Takođe, izvršeno je ispitivanje i poređenje<br />bioloških aktivnosti sintetisanih analoga sa sa aktivnošću i selektivnošću<br />kako GF i TF tako i doksorubicina, jedinjenja širokog spektra dejstva (DOX).<br />Hiralni prekursor novosintetisanih jedinjenja 1-15 bila je D-glukoza, a<br />jedinjenja 16 D-arabinoza.</p> / <p>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.</p>
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