Synthesis and antitumor potential of C19-derivatized steroidal D-homo lactones

Abstract

<p>U&nbsp; ovom&nbsp; radu&nbsp; ostvarene&nbsp; su&nbsp; sinteze C19-derivatizovanih&nbsp; steroidnih&nbsp; D-homo laktona.&nbsp; Takođe,&nbsp; sintetisani&nbsp; su&nbsp; i&nbsp; 5,6-halogeni derivati,&nbsp; 5,6-supstituisani&nbsp; kiseonični&nbsp; derivati,<br />kao&nbsp; i&nbsp; 6,19-epoksi&nbsp; steroidi.&nbsp; Za&nbsp; sva&nbsp; sintetisana jedinjenja&nbsp; je&nbsp; utvrđen&nbsp; antitumorski&nbsp; potencijal ispitivanjem&nbsp; njihove&nbsp; oralne&nbsp; bioraspoloživosti, antiproliferativne&nbsp; aktivnosti&nbsp; na&nbsp; &scaron;est&nbsp; ćelijskih linija&nbsp; kancera,&nbsp; vezivanja&nbsp; za&nbsp; odabrane&nbsp; steroidne receptore&nbsp; i&nbsp; inhibitorne&nbsp; aktivnosti&nbsp; na&nbsp; enzim AKR1C3.</p>

<p>In&nbsp; this&nbsp; paper,&nbsp; a&nbsp; synthesis&nbsp; of&nbsp; C19-derivatized steroidal D-homo lactones has been conducted. 5,6-Halogen derivatives, 5,6-substituted oxygen derivatives&nbsp; and&nbsp; 6,19-epoxy&nbsp; steroids&nbsp; were&nbsp; also synthesized.&nbsp; Antitumor&nbsp; potential&nbsp; was determined&nbsp; for&nbsp; all&nbsp; synthesized&nbsp; compounds&nbsp; by examining&nbsp; their&nbsp; oral&nbsp; bioavailability, antiproliferative activity on six cancer cell lines, binding&nbsp; to&nbsp; selected&nbsp; steroid&nbsp; receptors&nbsp; and inhibitor activity on the AKR1C3 enzyme.</p>