Oxazolinodoxorubicin - a promising new anthracycline.

Abstract:

: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.

journal_name

Anticancer Res

journal_title

Anticancer research

authors

Lukawska M,Klopotowska D,Milczarek M,Wietrzyk J,Studzian K,Szmigiero L,Porebska A,Oszczapowicz I

subject

Has Abstract

pub_date

2012-07-01 00:00:00

pages

2959-65

issue

7

eissn

0250-7005

issn

1791-7530

pii

32/7/2959

journal_volume

32

pub_type

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