Synthesis and biological evaluation of novel urea, thiourea and squaramide diastereomers possessing sugar backbone.
Carbohydr Res
; 492: 107991, 2020 Jun.
Article
in En
| MEDLINE
| ID: mdl-32259705
ABSTRACT
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, 1H NMR, 13C 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 µM 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 µM) against HeLa cell line. IC50 results also confirm these activities. The compounds 9, 10 and 11 have the IC50 values of 1.10 µM, 1.51 µM and 1.02 µM, respectively while 5-FU has 2.51 µM. Moreover, their cytotoxicity tests have proven that their viabilities were in between 50% and 100%.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Quinine
/
Urea
/
Esters
/
Sugars
/
Antineoplastic Agents
Limits:
Humans
Language:
En
Journal:
Carbohydr Res
Year:
2020
Document type:
Article
Affiliation country: