Structure-antitumor activity relationship of semi-synthetic Spicamycin derivatives

T Sakai; H Kawai; M Kamishohara; A Odagawa; A Suzuki; T Uchida; T Kawasaki; T Tsuruo; N Otake

doi:10.7164/antibiotics.48.1467

Structure-antitumor activity relationship of semi-synthetic Spicamycin derivatives

J Antibiot (Tokyo). 1995 Dec;48(12):1467-80. doi: 10.7164/antibiotics.48.1467.

Authors

T Sakai¹, H Kawai, M Kamishohara, A Odagawa, A Suzuki, T Uchida, T Kawasaki, T Tsuruo, N Otake

Affiliation

¹ Pharmaceutical Research Laboratory, Kirin Brewery Co, Ltd, Gunma, Japan.

PMID: 8557605
DOI: 10.7164/antibiotics.48.1467

Abstract

New derivatives of spicamycin modified at the fatty acid moieties of the molecule were synthesized and their structure-activity relationships were examined. The antitumor activity was greatly influenced by modification of the fatty acid moieties to tetradecadienoyl or dodecadienoyl analogues exhibiting better antitumor activity against COL-1 human colon cancer xenograft than SPM VIII.

MeSH terms

Animals
Antibiotics, Antineoplastic / biosynthesis
Antibiotics, Antineoplastic / chemistry*
Antibiotics, Antineoplastic / pharmacology*
Humans
Magnetic Resonance Spectroscopy
Mice
Mice, Nude
Neoplasm Transplantation
Purine Nucleosides / biosynthesis
Purine Nucleosides / chemistry
Purine Nucleosides / pharmacology
Streptomyces / metabolism
Structure-Activity Relationship

Substances

Antibiotics, Antineoplastic
Purine Nucleosides
septacidin