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Synthesis of novel dimers containing cholesterol and ergosterol using click reaction and their anti-proliferative effects

机译:使用咔哒反应及其抗增殖效应合成含胆固醇和Ergosterol的新型二聚体

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This study aimed to achieve the synthesis of dimers containing cholesterol and ergosterol using click reaction and to perform biologic evaluations. For this purpose, cholesterol and ergosterol were converted to their esters. Three ergosterol esters were reported as novel compounds. To be used as linkers, furan and thiophene derivatives containing azide groups were synthesized. Of these, 2,5-bis(azidomethyl)thiophene was reported to be a novel compound. The obtained compounds were converted to dimers using a click reaction and 12 novel dimers were obtained as a result. The synthesized compounds were examined to evaluate their biologic activity against MCF-7 and HT29 cancer cells and MEF healthy cells. As a result of the biologic evaluation, the most effective compound against the MCF-7 cancer cell line was [2,5-furandiylbis(methylene)]bis(cholest-5-en-3-yl1H-1,2,3-triazole-4-pentanoate) with 205.06 mu M concentration and [2,5-furandiylbis(methylene)]bis(ergosta-5,7,22-trien-3-yl1H-1,2,3-triazole-4-propanoate) with 159.5 mu M concentration was the most effective for the HT29 cancer cell line.
机译:本研究旨在使用点击反应来实现含胆固醇和Ergosterol的二聚体的合成,并进行生物学评价。为此目的,将胆固醇和Ergosterol转化为酯。将三种Ergosterol酯报告为新化合物。用作接头,合成含有叠氮基团的呋喃和噻吩衍生物。其中,据报道,2,5-双(氮杂甲基)噻吩是一种新化合物。使用咔哒反应将所得化合物转化为二聚体,结果获得12个新二聚体。检查合成化合物以评估对MCF-7和HT29癌细胞和MEF健康细胞的生物活性。作为生物学评价的结果,对MCF-7癌细胞系的最有效化合物是[2,5-呋喃(亚甲基)] BIS(胆固醇-5-烯-3-基1H-1,2,3-三唑) -4-戊烷)浓度205.06μm,[2,5-呋喃(亚甲基)] BIS(Ergosta-5,7,22- Trien-3-Y1H-1,2,3-三唑-4-丙酸盐) 159.5μm浓度对HT29癌细胞系最有效。

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