Synthesis of novel dimers containing cholesterol and ergosterol using click reaction and their anti-proliferative effects
Küçük Resim Yok
Tarih
2020
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Springer Wien
Erişim Hakkı
info:eu-repo/semantics/closedAccess
Özet
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. [GRAPHICS] .
Açıklama
Anahtar Kelimeler
Cholesterol, Ergosterol, Dimeric Sterols, Click Chemistry, Anti-Proliferative Effects, 1,2,3-Triazoles, Anticancer, Apoptosis, Catalysts
Kaynak
Monatshefte Fur Chemie
WoS Q Değeri
Q4
Scopus Q Değeri
Q3
Cilt
151
Sayı
5
