Antitumor activity and COMPARE analysis of bis-indole derivatives

被引：19

作者：

Andreani, Aldo ^{[1
]}

Burnelli, Silvia ^{[1
]}

Granaiola, Massimiliano ^{[1
]}

Leoni, Alberto ^{[1
]}

Locatelli, Alessandra ^{[1
]}

Morigi, Rita ^{[1
]}

Rambaldi, Mirella ^{[1
]}

Varoli, Lucilla ^{[1
]}

Landi, Laura ^{[2
]}

Prata, Cecilia ^{[2
]}

Dalla Sega, Francesco Vieceli ^{[2
]}

Caliceti, Cristiana ^{[2
]}

Shoemaker, Robert H. ^{[3
]}

机构：

[1] Univ Bologna, Dipartimento Sci Farmaceut, I-40126 Bologna, Italy

[2] Univ Bologna, Dipartimento Biochim G Moruzzi, I-40126 Bologna, Italy

[3] NCI, Div Canc Treatment & Diag, Screening Technol Branch, Dev Therapeut Program, Frederick, MD 21702 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2010年 / 18卷 / 09期

关键词：

Indole; Pyridine; Antitumor; Hollow fiber assay; COMPARE; NQO1; TUMOR-CELL-LINES; INHIBITORS; INDUCERS; NAD(P)H;

D O I：

10.1016/j.bmc.2010.03.063

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：

This paper reports the synthesis of new derivatives (formed by two indole systems separated by a central moiety) analogous of potent antitumor agents previously described. The activity of the bis-indoles bearing a pyridine core confirms the good result described in the previous paper and compound 4c was chosen for the first in vivo experiment (Hollow Fiber Assay). COMPARE analysis and structure-activity relationships were also considered. Contrary to data reported by other Authors, no correlations were found between antitumor activity and NQO1 induction. (c) 2010 Elsevier Ltd. All rights reserved.

引用

页码：3004 / 3011

页数：8

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