Synthesis and biological evaluation of novel urea, thiourea and squaramide diastereomers possessing sugar backbone
Yükleniyor...
Tarih
2020
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
ELSEVIER SCI LTD
Erişim Hakkı
info:eu-repo/semantics/closedAccess
Özet
A series of novel chiral 14 urea, thiourea and squaramide stereoisomers possessing carbohydrate backbones as well as amide functional groups was synthesized and characterized by their, H-1 NMR, C-13 NMR, FT-IR, HRMS, optical rotation, and melting points. Their antiproliferative activities were investigated against HeLa and PC3 cell lines. The compounds 9, 11 and 12 showed better activities at 25 mu M against PC3 cell line with respect to the standard 5-fluorouracil (5-FU). Especially, the compounds 9 and 11 showed higher activities than the standard 5-FU even at low concentration (5 mu M) against HeLa cell line. IC50 results also confirm these activities. The compounds 9, 10 and 11 have the IC50 values of 1.10 mu M, 1.51 mu M and 1.02 mu M, respectively while 5-FU has 2.51 mu M. Moreover, their cytotoxicity tests have proven that their viabilities were in between 50% and 100%.
Açıklama
Bulut, Adnan/0000-0001-9322-0325
Anahtar Kelimeler
Sugar, Urea, Thiourea, Squaramide, Antiproliferative activity, Cytotoxicity
Kaynak
CARBOHYDRATE RESEARCH
WoS Q Değeri
Q3
Scopus Q Değeri
Q2
Cilt
492
Sayı
Künye
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