2-arylnaphthyridin-4-ones as potent antitumor agents targeting tumorigenic cell lines

2-arylnaphthyridin-4-ones as potent antitumor agents targeting tumorigenic cell lines

In order to search for new antitumor drug candidates from 2-arylnaphthyridin-4-ones (ANs), we have designed and synthesized a series of 3'-hydroxy or 6-hydroxy derivatives of ANs. Following the antitumor activity screening, most of these compounds were found to exhibit significant activity. Amo...

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Hauptverfasser: LEE, KUO-HSIUNG, CHOU, LIN, CHANG, LINGU, HUANG, CHI-HUNG, TENG, CHE-MING, CHENG, YUNG-YI, HSU, MEI-HUA, HUANG, LI-JIAU, WU, TIAN-SHUNG, TSAI, MENG-TUNG, LIAO, CHIHANG, LIN, HUI-YI, LIU, CHIN-YU, WAY, TZONG-DER, KUO, SHENGU
Format: Patent
Sprache:chi ; eng
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Zusammenfassung:In order to search for new antitumor drug candidates from 2-arylnaphthyridin-4-ones (ANs), we have designed and synthesized a series of 3'-hydroxy or 6-hydroxy derivatives of ANs. Following the antitumor activity screening, most of these compounds were found to exhibit significant activity. Among them, 2-(3-hydroxyphenyl)-5-methyl-1,8-naphthyridin-4(1H)-one (67) was the most promising. In a preliminary action mechanism study, the treatment of Hep3B hepatoma cells with compound 67 reveals that its mechanism of action is affect on microtubule and metastasis-related proteins. Then, the corresponding phosphate prodrug (86) of compound 67 was tested against Hep3B xenograft nude mice model for antitumor activity.