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
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.