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

DOI: 10.1248/cpb.45.424

Source and publish data:

Chemical and Pharmaceutical Bulletin p. 424 - 426 (1997)

Update date:2022-08-03

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Authors:

Endo, Yasuyuki

Ohno, Michihiro

Takehana, Shunji

Driedger, Paul E.

Stabel, Silvia

Shudo, Koichi

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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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