Futalosine and Its Derivatives, New Nucleoside Analogs

Futalosine, a new nucleoside analog, was isolated from a fermentation broth of Streptomyces sp. MK359-NF1. Some chemical derivatives of futalosine were prepared. 6-O-Methylfutalosine methylester inhibited growth of HeLa-S3 cells in vitro (IC50=19.5μg/ml) in contrast to the weak activity of futalosin...

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Veröffentlicht in:	Chemical & pharmaceutical bulletin 1999/07/15, Vol.47(7), pp.1032-1034
Hauptverfasser:	HOSOKAWA, Nobuo, NAGANAWA, Hiroshi, KASAHARA, Takako, HATTORI, Seiko, HAMADA, Masa, TAKEUCHI, Tomio, YAMAMOTO, Shinobu, TSUCHIYA, Kayoko S., HORI, Makoto
Format:	Artikel
Sprache:	eng
Schlagworte:	Antibiotics, Antineoplastic - biosynthesis Antibiotics, Antineoplastic - chemistry Antibiotics, Antineoplastic - pharmacology Antineoplastic drugs. Cytokines Biological and medical sciences Biotechnology Chemical Phenomena Chemistry, Physical Chromatography, High Pressure Liquid Drug Screening Assays, Antitumor Fundamental and applied biological sciences. Psychology futalosine Health. Pharmaceutical industry HeLa Cells HeLa-S3 Humans Industrial applications and implications. Economical aspects Magnetic Resonance Spectroscopy nucleoside analog Nucleosides - biosynthesis Nucleosides - chemistry Nucleosides - pharmacology Production of active biomolecules Spectrophotometry, Ultraviolet Streptomyces Streptomyces - metabolism
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Zusammenfassung:	Futalosine, a new nucleoside analog, was isolated from a fermentation broth of Streptomyces sp. MK359-NF1. Some chemical derivatives of futalosine were prepared. 6-O-Methylfutalosine methylester inhibited growth of HeLa-S3 cells in vitro (IC50=19.5μg/ml) in contrast to the weak activity of futalosine. 6-O-Methylfutalosine methylester at concentrations higher than 10μg/ml inhibited incorporation of 3H-TdR and 3H-UR but not 3H-Leu into the acid-soluble fractions of HeLa-S3 cells.
ISSN:	0009-2363 1347-5223
DOI:	10.1248/cpb.47.1032