当前位置： SCI文献检索 > BIOORGANIC & MEDICINAL CHEMISTRY LETTERS期刊下所有文献 > Antitumor platinum(II) complexes of N-cyclobutyl-1R,2R-diaminocyclohexane with dicarboxylates as leaving groups.

Antitumor platinum(II) complexes of N-cyclobutyl-1R,2R-diaminocyclohexane with dicarboxylates as leaving groups.

Abstract：

:Four platinum(II) complexes of N-cyclobutyl-1R,2R-diaminocyclohexane with different bidentate dicarboxylates (1 oxalate, 2 malonate, 3 1,1-cyclobutanedicarboxylate and 4 3-hydroxy-1,1-cyclobutanedicarboxylate) as leaving groups were synthesized and characterized by elemental analyses, IR and (1)HNMR spectra together with ESI-MS spectroscopy. All complexes showed considerable cytotoxicity against the tested four human tumor cell lines including A549, HCT-116, HepG-2 and MCF-7. Especially, complex 4 showed good cytotoxicity against A549 (IC50=3.5μM) and HCT-116 (IC50=0.9μM) cancer cell lines. Moreover, complex 3 is the most effective agent among the tested compounds against MCF-7 cell line (IC50=1.1μM). The DNA binding behavior of both complexes 3 and 4, studied by agarose gel electrophoresis, revealed that they bound to DNA in almost the same way as cisplatin.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Xu G,Zhao J,Gou S,Pang J

doi

10.1016/j.bmcl.2014.11.069

subject

Has Abstract

pub_date

2015-01-15 00:00:00

pages

221-4

issue

2

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(14)01264-5

journal_volume

25

pub_type

杂志文章

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