Evaluation of antitumor properties of novel saframycin analogs in vitro and in vivo

被引：18

作者：

Spencer, Jeffrey R.

Sendzik, Martin

Oeh, Jason

Sabbatini, Peter

Dalrymple, Stacie A.

Magill, Catherine

Kim, Hyunjin M.

Zhang, Penglie

Squires, Neil

Moss, Katherine G.

Sukbuntherng, Juthamas

Graupe, Doris

Eksterowicz, John

Young, Peter R.

Myers, Andrew G.

Green, Michael J.

机构：

[1] Celera Genom, San Francisco, CA 94080 USA

[2] Harvard Univ, Dept Chem & Chem Biol, Cambridge, MA 02128 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 18期

关键词：

saframycin analog; GI50; DNA binding; fluorescence; in vivo model;

D O I：

10.1016/j.bmcl.2006.06.085

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Novel analogs of (-)-saframycin A are described. The analogs are shown to be potent inhibitors of the in vitro growth of several tumor cells in a broad panel and promising as leads for further optimization. The first in vivo studies in a solid tumor model (HCT-116) reveal potent antitumor activity with associated toxicity of daily administration. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：4884 / 4888

页数：5

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