Role of the Hydrophobic Moiety of Tumor Promoters. Synthesis and Activity of Benzolactams with Alkyl Substituents at Various Positions.

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  • Role of the Hydrophobic Moiety of Tumor

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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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