Synthesis of new phorbol derivatives having ethereal side chain and evaluation of their anti-HIV activity

被引：17

作者：

Matsuya, Y

Yu, Z

Yamamoto, N

Mori, M

Saito, H

Takeuchi, M

Ito, M

Nemoto, H

机构：

[1] Toyama Med & Pharmaceut Univ, Fac Pharmaceut Sci, Toyama 9300914, Japan

[2] Tokyo Med & Dent Univ, Dept Microbiol, Bunkyo Ku, Tokyo 1138519, Japan

[3] Lead Chem Co Ltd, Toyama 9300912, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2005年 / 13卷 / 14期

关键词：

phorbol; anti-HIV agents; ethereal side chain; safety index;

D O I：

10.1016/j.bmc.2005.04.056

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Several new phorbol derivatives having ethereal substituents at the 12-position were synthesized and subjected to biological evaluation to find new candidates of an anti-HIV agent. Among them, 12-O-(methoxymethyl)phorbol 13-decanoate showed potent inhibitory activity against infection of HIV-1 in MT-4 cells (EC50: 1.3 ng/mL) and relatively low cytotoxicity (CC50: 8.3 mu g/mL). This compound was also found to have sufficient stability in mouse plasma compared with the corresponding 12-acetate derivative, which was an equipotent HIV-1 inhibitor, but with an activity that decreased considerably after plasma treatment. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：4383 / 4388

页数：6

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