ROLE OF THE HYDROPHOBIC MOIETY OF TUMOR PROMOTERS. SYNTHESIS AND ACTIVITY OF BENZOLACTAMS WITH ALKYL SUBSTITUENTS AT VARIOUS POSITIONS

Yasuyuki ENDO; Michihiro OHNO; Shunji TAKEHANA; Paul E. DRIEDGER; Silvia STABEL; Koichi SHUDO

doi:10.1248/cpb.45.424

Yasuyuki ENDO, Michihiro OHNO, Shunji TAKEHANA, Paul E. DRIEDGER, Silvia STABEL, Koichi SHUDO

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Keywords: tumor promoter, teleocidin, benzolactam, structure-activity relation, hydrophobic interaction

JOURNAL FREE ACCESS

1997 Volume 45 Issue 2 Pages 424-426

DOI https://doi.org/10.1248/cpb.45.424

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Abstract

We synthesized benzolactams with hydrophobic substituents at various positions as analogs of (-)-benzolactam-V8-310 ((-)-BL-V8-310, 1) which reproduces the active conformation and biological activity of teleocidins. Structure-activity data indicate that the existence of a hydrophobic region between C-2 and C-9, and the steric factor at C-8 play critical roles in the appearance of biological activities.

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