RT Journal Article
SR Electronic
T1 Oxazolinodoxorubicin – a Promising New Anthracycline
JF Anticancer Research
JO Anticancer Res
FD International Institute of Anticancer Research
SP 2959
OP 2965
VO 32
IS 7
A1 LUKAWSKA, MALGORZATA
A1 KLOPOTOWSKA, DAGMARA
A1 MILCZAREK, MAGDALENA
A1 WIETRZYK, JOANNA
A1 STUDZIAN, KAZIMIERZ
A1 SZMIGIERO, LESZEK
A1 POREBSKA, ANNA
A1 OSZCZAPOWICZ, IRENA
YR 2012
UL http://ar.iiarjournals.org/content/32/7/2959.abstract
AB Oxazolinodoxorubicin, a doxorubicin analog with a modified daunosamine moiety was synthesized. The properties of this compound and the parent doxorubicin were compared. The cytotoxicity in vitro studies against several human tumor cell lines (PC-3, MCF-7, SW707, HL-60, RPMI 8226, ACHN) showed higher antiproliferative potency for this new compound. Moreover, its ability to completely overcome the drug resistance of cancer cells in vitro was revealed (LoVo, LoVo/DX, MES-SA, MES-SA/DX5, HL-60, HL-60/Vinc, HL-60/MX2 cell lines). Cellular uptake analyzed on HL-60 and HL-60/MX2 cells, demonstrated higher penetration levels of oxazolinodoxorubicin compared to that of doxorubicin. In animal experiments, general toxicity of oxazolinodoxorubicin was lower than that observed for doxorubicin. Furthermore, similar antitumor effects was observed in NOD/SCID mice bearing resistant HL-60/Vinc leukemia tumor and in mice treated with the new or parent compounds. The presented results suggest that oxazolinodoxorubicin is a new anthracycline with an advantageous biological activity profile.