Structure-activity relationships in the acronycine and benzo[b]acronycine series: Role of the pyran ring

被引：9

作者：

Do, Quyen ^{[1
]}

Mai, Huong Doan Thi ^{[1
]}

Gaslonde, Thomas ^{[1
]}

Pfeiffer, Bruno ^{[2
]}

Leonce, Stephane ^{[2
]}

Pierre, Alain ^{[2
]}

Michel, Sylvie ^{[1
]}

Tillequin, Francois ^{[1
]}

Dufat, Hanh ^{[1
]}

机构：

[1] Univ Paris 05, Lab Pharmacognosie, UMR CNRS 8638, Fac Pharm, F-75006 Paris, France

[2] Inst Rech Servier, Div Rech Cancerol, F-78290 Croissy Sur Seine, France

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 43卷 / 12期

关键词：

Acridone; Benzo[b]acridone; Acronycine; Cytotoxicity;

D O I：

10.1016/j.ejmech.2008.01.033

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In order to explore the structure-activity relationships in the acronycine series, simplified analogues of cis-1,2-diacetoxy-1,2-dihydroacronycine and cis-1,2-diacetoxy-1,2-dihydrobenzo[b]acronycine (S23906-1, under clinical trials) lacking the fused pyran ring, but possessing an acetoxymethyl leaving group at position 4 were prepared. These new analogues only displayed marginal antiproliferative activity compared to the parent compounds. The presence of the angularly fused dimethylpyran ring appears as an indispensable structural requirement to observe significant cytotoxic activity in this series. (C) 2008 Elsevier Masson SAS. All fights reserved.

引用

页码：2677 / 2687

页数：11

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