SYNTHESIS AND BIOLOGICAL-ACTIVITIES OF FLUORINE-SUBSTITUTED (-)-INDOLACTAM-V, THE CORE STRUCTURE OF TUMOR PROMOTER TELEOCIDINS

Citation
S. Okuno et al., SYNTHESIS AND BIOLOGICAL-ACTIVITIES OF FLUORINE-SUBSTITUTED (-)-INDOLACTAM-V, THE CORE STRUCTURE OF TUMOR PROMOTER TELEOCIDINS, Bioorganic & medicinal chemistry letters, 4(3), 1994, pp. 431-434
Citations number
22
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
ISSN journal
0960894X
Volume
4
Issue
3
Year of publication
1994
Pages
431 - 434
Database
ISI
SICI code
0960-894X(1994)4:3<431:SABOF(>2.0.ZU;2-I
Abstract
To investigate the conformation-activity relationship, new indolactam derivatives with a fluorine atom at position 5 or 6 were synthesized. (-)-5-Fluoroindolactam-V (2) existing mainly as the sofa conformer in solution was far less biologically active than (-)-6-fluoroindolactam- V (3) existing mainly as the twist conformer. This suggests that the s ofa conformation of (-)-indolactam-V (1) is not a biologically active form.