Sinteza i antitumorski potencijal C19-derivatizovanih steroidnih D-homo laktona

Abstract

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

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