Role of the hydrophobic moiety of tumor promoters. Synthesis and activity of benzolactams with alkyl substituents at various positions

Article abstract of DOI:10.1248/cpb.45.424

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.

Full text of DOI:10.1248/cpb.45.424

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