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Synthesis and cytotoxicity of (-)-renieramycin G analogs.

Abstract：

:(-)-Renieramycin G and fifteen C-22 analogs were prepared employing l-tyrosine as the chiral starting material. These analogs, along with (-)-renieramycin G itself, were evaluated in vitro for cytotoxicity against HCT-8, BEL-7402, A2780, MCF-7, A549, BGC-823, Ketr3, KB, Hela cells. The IC(50) values of most of these analogs were at the level of μM. Among these analogs, 2-thiophenecarboxylate ester derivative 17 exhibited potent cytotoxic activity against KB cell line with the IC(50) of 20 nM. From this study, it could be concluded that the C-22 side chain played an important role in the cytotoxic potency and specificity of this class of (-)-renieramycin G derivatives.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Liu W,Dong W,Liao X,Yan Z,Guan B,Wang N,Liu Z

doi

10.1016/j.bmcl.2011.01.025

subject

Has Abstract

pub_date

2011-03-01 00:00:00

pages

1419-21

issue

5

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)00038-2

journal_volume

21

pub_type

杂志文章

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