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Evaluation of novel aryloxyalkyl derivatives of imidazole and 1,2,4-triazole as heme oxygenase-1 (HO-1) inhibitors and their antitumor properties.

Abstract：

:A novel series of aryloxyalkyl derivatives of imidazole and 1,2,4-triazole, 17-31, was designed and synthesized as inhibitors of heme oxygenase-1 (HO-1) and heme oxygenase-2 (HO-2). Some of these compounds were found to be good inhibitors of HO-1, in particular those carrying an imidazole moiety as azolyl group and a 3-bromo or 4-iodophenyl as aryl moiety. The most potent compounds 6 and 30 were selected and studied for their antitumor properties in a model of LAMA-84 R cell line overexpressing HO-1 and resistant to imatinib mesylate (IM), a tyrosine-kinase inhibitor used in the treatment of multiple types of cancer, most notably Philadelphia Chromosome positive (Ph(+)) Chronic Myelogenous Leukemia (CML). Results show that both 6 and 30 sensitized LAMA-84 R cell line to antitumor properties of IM.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Salerno L,Pittalà V,Romeo G,Modica MN,Siracusa MA,Di Giacomo C,Acquaviva R,Barbagallo I,Tibullo D,Sorrenti V

doi

10.1016/j.bmc.2013.06.040

subject

Has Abstract

pub_date

2013-09-01 00:00:00

pages

5145-53

issue

17

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(13)00571-3

journal_volume

21

pub_type

杂志文章

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