Synthesis and Biological Activities of New Conformationally Restricted Analogues of (-)-Indolactam-V: Elucidation of the Biologically Active Conformation of the Tumor-Promoting Teleocidins.-In order to indentify the active conformation of the title compounds the new twist-restricted analogues (I) and (II) along with sofa-restricted ones (III) their activities are evaluated in three in vitro bioassays associated with in vivo tumor-promoting activity. The results reveal that the active conformation is close to the twist form of cis amide, not to the sofa form of trans amide. Introduction of a prenyl group into (Ia) and (IIa) significantly enhances the activity, while sofa-restricted (IIIb) shows only very weak activity. Thus the active conformation of the title compounds is close to the twist form. -(IRIE, K.; ISAKA, T.; IWATA, Y.; YANAI, Y.; NAKAMURA, Y.; KOIZUMI, F.; OHIGASHI, H.; WENDER, P. A.; SATOMI, Y.; NISHINO, H.; J. Am. Chem.
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