1. Synthesis and studies of acetylthioglycoside conjugates of 4-chloro-1,2-dithiole-3-thione as potential antitumor agents
- Author
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Oleg A. Rakitin, Yu. E. Sabutskii, Vladimir A. Ogurtsov, Sergey G. Polonik, Roman S. Popov, Sergey N. Fedorov, Alexandra S. Kuzmich, and Alla G. Guzii
- Subjects
Human leukemia ,Transcriptional activity ,integumentary system ,010405 organic chemistry ,Chemistry ,Chlorine atom ,Cancer ,General Chemistry ,010402 general chemistry ,medicine.disease ,01 natural sciences ,Combinatorial chemistry ,0104 chemical sciences ,Soft agar ,3h 1 2 dithiole 3 thione ,medicine ,Nucleophilic substitution ,Conjugate - Abstract
Nucleophilic substitution of a chlorine atom in 4,5 dichloro-1,2-dithiole-3-thione with per-O-acetyl-1-mercaptho derivatives of d-glucose, d-galactose, d-mannose, d-xylose, l-arabinose, and d-maltose gave six new acetylthioglycoside conjugates of 4-chloro-1,2-dithiole-3-thione. These thioglycosides were shown to possess cancer preventive activity on the models of JB6 Cl41 P+ mouse epidermal cells and THP-1 human leukemia cells in soft agar, as well as to inhibit the AP-1-dependent transcriptional activity in JB6 Cl41 luc-AP-1 cells, which suggests the possibility of using the new compounds as potential cancer preventive drugs.
- Published
- 2021