Synthesis and biological activities of NB-506 analogues modified at the glucose group

A new indolocarbazole compound, NB-506 ( 1 ), modified at the glucose group yielded a β- d-glucopyranoside, J-107,088 ( 2 ), which showed potent anticancer activity. A β- d-ribofuranoside, J-109,534 ( 3 ), was found to be 6 times more potent than J-107,088 at inhibiting topoisomerase I.

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2000-03, Vol.10 (5), p.419-422
Hauptverfasser:	Ohkubo, Mitsuru, Nishimura, Teruyuki, Kawamoto, Hiroshi, Nakano, Masato, Honma, Teruki, Yoshinari, Tomoko, Arakawa, Hiroharu, Suda, Hiroyuki, Morishima, Hajime, Nishimura, Susumu
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic agents Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacology Biological and medical sciences Carbazoles - chemical synthesis Carbazoles - pharmacology Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology General aspects Glucose - chemistry Glucosides - chemical synthesis Glucosides - pharmacology Humans Indoles Magnetic Resonance Spectroscopy Mass Spectrometry Medical sciences Pharmacology. Drug treatments Stereoisomerism Topoisomerase I Inhibitors Tumor Cells, Cultured
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Beschreibung
Zusammenfassung:	A new indolocarbazole compound, NB-506 ( 1 ), modified at the glucose group yielded a β- d-glucopyranoside, J-107,088 ( 2 ), which showed potent anticancer activity. A β- d-ribofuranoside, J-109,534 ( 3 ), was found to be 6 times more potent than J-107,088 at inhibiting topoisomerase I.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(00)00004-4