Anti-AIDS agents .28. Synthesis and anti-HIV activity of methoxy substituted 3',4'-Di-O-(-)-camphanoyl-(+)-cis-khellactone (DCK) analogues

被引：41

作者：

Takeuchi, Y

Xie, L

Cosentino, LM

Lee, KH

机构：

[1] UNIV N CAROLINA,SCH PHARM,DIV MED CHEM & NAT PROD,NAT PROD LAB,CHAPEL HILL,NC 27599

[2] BIOTECH RES LABS INC,ROCKVILLE,MD 20850

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(97)10050-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Four isomeric methoxy substituted DCK analogues (3-6) were asymmetrically synthesized from different starting materials. 5-Methoxy-3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (5) exhibited extremely potent anti-HIV activity against HIV-1 replication in H9 lymphocyte cells with EC50 and therapeutic index values of 0.00038 mu M and >402,632, respectively, which are better than those of DCK and AZT in this assay. (C) 1997 Elsevier Science Ltd.

引用

页码：2573 / 2578

页数：6

共 7 条

[1]

AHLUWALIA VK, 1977, INDIAN J CHEM B, V15, P945

[2]

HASHIMOTO F, IN PRESS MED CHEM

[3]

HLUBUEK J, 1971, AUST J CHEM, V62, P2347

[4] ANTI-AIDS AGENTS .14. 3',4'-DI-O-(-)-CAMPHANOYL-(+)-CIS-KHELLACTONE AND RELATED-COMPOUNDS - A NEW CLASS OF POTENT ANTI-HIV AGENTS [J].