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Synthesis of the new pseudo-symmetrical tamoxifen derivatives and their anti-tumor activity.

Abstract：

:Three new pseudo-symmetrical tamoxifen derivatives, RID-B (15), C (16), and D (17), were synthesized via the novel three-component coupling reaction, and the structure-activity relationships of the pseudo-symmetrical tamoxifen derivatives were examined. It was discovered that 15 strongly inhibits the viability of HL-60 human acute promyelocytic leukemia, whereas 16 possesses medium activity against the cell line and 17 has no effect on the cell viability. The agarose gel electrophoresis for DNA cleavage showed the cell death might be induced by apoptosis.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Shiina I,Sano Y,Nakata K,Kikuchi T,Sasaki A,Ikekita M,Hasome Y

doi

10.1016/j.bmcl.2007.02.037

subject

Has Abstract

pub_date

2007-05-01 00:00:00

pages

2421-4

issue

9

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(07)00235-1

journal_volume

17

pub_type

杂志文章

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