Seven-membered ring azasugars as glycosidase inhibitors and anticancer agents

Authors
Lohray, BB Bhushan, V Prasuna, G Jayamma, Y Raheem, MA Papireddy, P Umadevi, B Premkumar, M Lakshmi, NS Narayanareddy, K
Citation
Bb. Lohray et al., Seven-membered ring azasugars as glycosidase inhibitors and anticancer agents, I J CHEM B, 38(12), 1999, pp. 1311-1321
Citations number
49
Categorie Soggetti
Organic Chemistry/Polymer Science
Journal title
INDIAN JOURNAL OF CHEMISTRY SECTION B-ORGANIC CHEMISTRY INCLUDING MEDICINAL CHEMISTRY
ISSN journal
03764699 → ACNP
Volume
38
Issue
12
Year of publication
1999
Pages
1311 - 1321
Database
ISI
SICI code
0376-4699(199912)38:12<1311:SRAAGI>2.0.ZU;2-L
Abstract
Synthesis of various C-2 symmetrical tetrahydroxyazepanes has been reported by the reaction of bisepoxides with various primary amines. The tetrahydro xyazepanes inhibit beta-glucosidases in micromolar range and also exhibit a nticancer activity in various cancer cell lines with GI(50) values in the r ange of 2 to 9x10(-5) M. The azepanes are poor inhibitors of HIV protease a nd their IC50 values are in the range 2x10(-4) M.