Synthesis of Benzoxazole Derivatives and Investigation of Their mTOR Inhibitor Activities

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Çolak S., Gürsoy Ş., Kuzu B., Türkmenoğlu B., Burmaoğlu S., Algül Ö.

12. International Drug Chemistry Conference, Antalya, Turkey, 7 - 10 March 2024, pp.104-108

  • Publication Type: Conference Paper / Full Text
  • City: Antalya
  • Country: Turkey
  • Page Numbers: pp.104-108
  • Erzincan Binali Yildirim University Affiliated: Yes


This study presents the synthesis of a series of novel chalcone-hybrid derivatives employing a two-step reaction scheme. Initially, 1,2,3,4-tetrasubstituted pyrrole derivatives were synthesized in a one-pot three-component reaction, utilizing suitable primary amines, 1,3-dicarbonyl compounds, and trans-β-nitrostyrene at ambient temperature. Subsequently, chalcone-pyrrole hybrid compounds were prepared in the second step, utilizing the obtained 1,2,3,4-tetrasubstituted pyrrole derivatives and substituted benzaldehyde derivatives in basic media, resulting in yields ranging from high to excellent. The synthesized compounds underwent comprehensive spectroscopic analysis for characterization purposes. Subsequently, their anti-proliferative activities were assessed against breast cancer cell lines, MCF7 and MDA-MB-231, employing the MTT assay, revealing moderate to high activity levels. Furthermore, the compounds were subjected to in silico analysis, wherein the binding modes of the active molecules were elucidated through molecular docking studies.