Dizajn, sinteza i antiproliferativna aktivnost prirodnih citotoksičnih laktona i analoga

Srećo Zelenović, Bojana

Design, synthesis and antiproliferative activity ofnatural cytotoxic lactones and analogues

Abstract

Ostvarene su višefazne sinteze prirodnih citotoksičnih laktona (+)-murikatacina (1), (–)-murikatacina (ent-1) i (+)-goniofufurona (2), kao i njihovih novih analoga (3a, 4, 5, 6, 7, 8, 9, ent-7 i ent-9), polazeći iz D-ksiloze ili iz D-glukoze. Ispitana je in vitro citotoksična aktivnost sintetizovanih prirodnih proizvoda i analoga prema odabranim humanim tumorskim ćelijskim linijama (K562, HL-60, Jurkat, Raji, HT-29, MDA-MB 231 i HeLa), kao i prema ćelijama fetalnih fibroblasta pluća (MRC-5).

Multiphase synthesis of natural cytotoxic lactones (+)-muricatacin (1), (–)-muricatacin (ent-1) and (+)-goniofufurone (2), as well as synthesis of their analogues (3a, 4, 5, 6, 7, 8, 9, ent-7and ent-9) was achived from D-xylose or D-glucose as starting compounds. In vitro cytotoxic activity of synthetized natural products and analogues against selected human tumour cell lines (K562, HL-60, Jurkat, Raji, HT-29, MDA-MB 231 and HeLa) and against cells of natural foetal lung fibroblasts (MRC-5) was examined.

Faculty:
University of Novi Sad, Faculty of Science
Date:
28-02-2013

Keywords:

Citotoksični laktoni / Cytotoxic lactones / goniofufuron / murikatacin / kardiobutanolid / sinteza analoga / SAR / antiproliferativna aktivnost / goniofufurone / muricatacin / cardiobutanolide / analogues synthesis / SAR / antiproliferative activity

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