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Titolo:
DESIGN, SYNTHESIS AND BIOLOGICAL-ACTIVITY OF PROTAXOLS
Autore:
NICOLAOU KC; RIEMER C; KERR MA; RIDEOUT D; WRASIDLO W;
Indirizzi:
SCRIPPS CLIN & RES INST,DEPT CHEM,10666 N TORREY PINES RD LA JOLLA CA92037 UNIV CALIF SAN DIEGO,DEPT CHEM LA JOLLA CA 92093 SCRIPPS CLIN & RES INST,DEPT MOLEC BIOL LA JOLLA CA 92037 SCRIPPS CLIN & RES INST,DRUG DISCOVERY UNIT LA JOLLA CA 92037
Titolo Testata:
Nature
fascicolo: 6436, volume: 364, anno: 1993,
pagine: 464 - 466
SICI:
0028-0836(1993)364:6436<464:DSABOP>2.0.ZU;2-9
Fonte:
ISI
Lingua:
ENG
Soggetto:
WATER-SOLUBLE PRODRUGS; ANTITUMOR-ACTIVITY; TAXOL; CELLS; MICROTUBULES; AGENTS; ASSAY;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
17
Recensione:
Indirizzi per estratti:
Citazione:
K.C. Nicolaou et al., "DESIGN, SYNTHESIS AND BIOLOGICAL-ACTIVITY OF PROTAXOLS", Nature, 364(6436), 1993, pp. 464-466

Abstract

TAXOL1-6 is a product isolated from the Pacific yew tree (Taxus brevifolia) and is a potent microtubule-stabilizing agent which has recently been approved for treatment of otherwise intractable ovarian cancer. Despite taxol's therapeutic promise, its aqueous insolubility (<0.004mg ml-1) hampers its clinical application. Here we report the design,synthesis and biological activity of a series of taxol-releasing compounds (protaxols) with improved pharmacological properties. These prodrugs were designed to increase their aqueous solubility and allow for taxol release under basic or physiological conditions. We demonstrate the stability of these prodrugs at pH less-than-or-equal-to 7 and their ability to release taxol in a basic medium. Taxol-like microtubule-stabilizing activity7-9 appears after the release of taxol. In vitro these prodrugs have cytotoxic properties against tumour cell lines comparable to those of taxol; moreover, human plasma catalyses the release of active taxol. These protaxols have greater potential as anticancer agents than the parent compounds taxol and taxotere (Fig. 1a).

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 16/07/20 alle ore 06:11:52