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Synthesis and preliminary evaluation steroidal antiestrogen-geldanamycin conjugates.

Abstract：

:Three novel steroidal antiestrogen-geldanamycin conjugates were prepared using a convergent strategy. The antiestrogenic component utilized the 11β-(4-functionalized-oxyphenyl) estradiol scaffold, while the geldanamycin component was derived by replacement of the 17-methoxy group with an appropriately functionalized amine. Ligation was achieved in high yield using azide alkyne cyclization reactions. Evaluation of the products against two breast cancer cell lines indicated that the conjugates retained significant antiproliferative activity.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Adam Hendricks J,Hanson RN,Amolins M,Mihelcic JM,Blagg BS

doi

10.1016/j.bmcl.2013.03.116

subject

Has Abstract

pub_date

2013-06-15 00:00:00

pages

3635-9

issue

12

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(13)00444-7

journal_volume

23

pub_type

信件

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