Design and Synthesis of C-Ring Lactone- and Lactam-Based Podophyllotoxin Analogues as Anticancer Agents

被引：17

作者：

Singh, Pragya ^{[1
]}

Faridi, Uzma ^{[1
]}

Srivastava, Suchita ^{[1
]}

Kumar, Jonnala Kotesh ^{[1
]}

Darokar, Mahender Pandurang ^{[1
]}

Luqman, Suaib ^{[1
]}

Shanker, Karuna ^{[1
]}

Chanotiya, Chandan Singh ^{[1
]}

Gupta, Atul ^{[1
]}

Gupta, Madan Mohan ^{[1
]}

Negi, Arvind Singh ^{[1
]}

机构：

[1] CSIR, CIMAP, Lucknow 226015, Uttar Pradesh, India

来源：

CHEMICAL & PHARMACEUTICAL BULLETIN | 2010年 / 58卷 / 02期

关键词：

podophyllotoxin; anticancer; osmotic fragility; MTT assay; DNA TOPOISOMERASE-II; ANTITUMOR AGENTS; POTENT INHIBITORS; DERIVATIVES; 4'-O-DEMETHYLEPIPODOPHYLLOTOXIN; CELLS;

D O I：

10.1248/cpb.58.242

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel podophyllotoxin (PDT) analogues was synthesized in which the lactone moiety was shifted to C ring. Some of the derivatives were also synthesized with modified A ring. Analogues 23 and 25 exhibited potent in vitro cytotoxicity against colon cancer (CaCO2) cell line. p-Demethylated E-ring analogues exhibited better potency than the corresponding methylated analogues. These analogues showed toxicity comparable to PDT against human erythrocytes albeit at much higher concentrations (100,mu g/ml) than their cytotoxicity values.

引用

页码：242 / 246

页数：5

共 15 条

[1]

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[2] Antitumor agents .163. Three-dimensional quantitative structure-activity relationship study of 4'-O-demethylepipodophyllotoxin analogs using the modified CoMFA/q(2)-GRS approach [J].