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Titolo:
A synthetic triptycene bisquinone, which blocks nucleoside transport and induces DNA fragmentation, retains its cytotoxic efficacy in daunorubicin-resistant HL-60 cell lines
Autore:
Wang, BN; Wu, MF; Perchellet, EM; McIlvain, CJ; Sperfslage, BJ; Huang, XD; Tamura, M; Stephany, HA; Hua, DH; Perchellet, JP;
Indirizzi:
Kansas State Univ, Div Biol, Anti Canc Drug Lab, Manhattan, KS 66506 USA Kansas State Univ Manhattan KS USA 66506 rug Lab, Manhattan, KS 66506 USA Kansas State Univ, Dept Chem, Manhattan, KS 66506 USA Kansas State Univ Manhattan KS USA 66506 pt Chem, Manhattan, KS 66506 USA
Titolo Testata:
INTERNATIONAL JOURNAL OF ONCOLOGY
fascicolo: 6, volume: 19, anno: 2001,
pagine: 1169 - 1178
SICI:
1019-6439(200112)19:6<1169:ASTBWB>2.0.ZU;2-N
Fonte:
ISI
Lingua:
ENG
Soggetto:
BIFUNCTIONAL ANTICANCER DRUGS; MULTIDRUG-RESISTANCE; HL60 CELLS; IN-VITRO; ADRIAMYCIN RESISTANCE; P-GLYCOPROTEIN; LEUKEMIC-CELLS; DIPYRIDAMOLE ANALOGS; GENE-EXPRESSION; NANOMOLAR RANGE;
Keywords:
triptycene bisquinone; sensitive and multidrug-resistant HL-60 cells; tumor cell growth and viability; DNA synthesis; nucleoside transport; DNA cleavage;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
57
Recensione:
Indirizzi per estratti:
Indirizzo: Perchellet, JP Kansas State Univ, Div Biol, Anti Canc Drug Lab, Ackert Hall, Manhattan, KS 66506 USA Kansas State Univ Ackert Hall Manhattan KS USA 66506 06 USA
Citazione:
B.N. Wang et al., "A synthetic triptycene bisquinone, which blocks nucleoside transport and induces DNA fragmentation, retains its cytotoxic efficacy in daunorubicin-resistant HL-60 cell lines", INT J ONCOL, 19(6), 2001, pp. 1169-1178

Abstract

In contrast to the parent triptycene (code name TTO), triptycene bisquinone (code name TT2) is cytostatic (IC50: 300 nM) and cytotoxic (IC50: 230 nM)in wild-type (WT), drug-sensitive HL-60 cells (HL-60-S) at day 4. Therefore, the effects of this new quinone antitumor drug were assessed and compared to those of daunorubicin (DAU, daunomycin) in the multidrug-resistant (MDR) HL-60-RV and HL-60-R8 sublines, which respectively overexpress P-glycoprotein (P-gp) or multidrug resistance-associated protein (MRP). In contrast to DAU, which loses its cytostatic [resistance factors (RFs): 22.9-35.7] and cytotoxic (RFs: 23.8-31.3) activities in MDR sublines, TT2 decreases tumor cell proliferation (R-Fs: 0.9-1.3) and viability (RFs: 0.9-1.5) as effectively in HL-60-S as in HL-60-RV and HL-60-R8 cells at days 2 and 4. Similarly, DAU inhibits the rate of DNA synthesis less effectively in MDR than in parental HL-60 cells (R-Fs: 8.1-11.9) but TT2 decreases the incorporation of (3)[H]-thymidine into DNA to the same degree in HL-60-S.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 14/07/20 alle ore 10:13:16