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Synthesis and anticancer activity of benzyloxybenzaldehyde derivatives against HL-60 cells.

Abstract：

:A series of benzyloxybenzaldehyde derivatives were prepared and tested against the HL-60 cell line for anticancer activity. Preliminary structure-activity relationships were established. It was discovered that 2-(benzyloxy)benzaldehyde (17), 2-(benzyloxy)-4-methoxybenzaldehyde (26), 2-(benzyloxy)-5-methoxybenzaldehyde (27), 2-(benzyloxy)-5-chlorobenzaldehyde (28), 2-[(3-methoxybenzyl)oxy]benzaldehyde (29), 2-[(2-chlorobenzyl)oxy]benzaldehyde (30), and 2-[(4-chlorobenzyl)oxy]benzaldehyde (31) exhibited significant activity at 1-10 microM. Among them, compound 29 was the most potent one. The morphological assessment and DNA fragmentation analysis indicated that these compounds arrested cell cycle progression at G2/M phase and induced cell apoptosis. They resulted in the loss of mitochondrial membrane potential after 12h of treatment.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Lin CF,Yang JS,Chang CY,Kuo SC,Lee MR,Huang LJ

doi

10.1016/j.bmc.2004.12.026

subject

Has Abstract

pub_date

2005-03-01 00:00:00

pages

1537-44

issue

5

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(04)01010-7

journal_volume

13

pub_type

杂志文章

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