Antiproliferative and Proapoptotic Activities of a New Class of Pyrazole Derivatives in HL-60 Cells

被引：36

作者：

Anzaldi, Maria ^{[1
]}

Maccio, Chiara ^{[1
]}

Mazzei, Mauro ^{[1
]}

Bertolotto, Maria ^{[2
]}

Ottonello, Luciano ^{[2
]}

Dallegri, Franco ^{[2
]}

Balbi, Alessandro ^{[1
]}

机构：

[1] Univ Genoa, Dipartimento Sci Farmaceut, I-16132 Genoa, Italy

[2] Univ Genoa, Dipartimento Med Interna, Clin Med Interna 1, I-16132 Genoa, Italy

来源：

CHEMISTRY & BIODIVERSITY | 2009年 / 6卷 / 10期

关键词：

ANTIBACTERIAL ACTIVITY; INHIBITORS; APOPTOSIS; ANTITUMOR; RETINOIDS; MOLECULE; AGENTS;

D O I：

10.1002/cbdv.200800354

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

070307 [化学生物学]; 071010 [生物化学与分子生物学];

摘要：

A series of N-substituted pyrazole derivatives have been synthesized and tested for their anticancer effect on the HL-60 leukaemia cell line. Four were active both in cell-growth inhibition and in inducing apoptosis. The inhibition of cell growth mainly reflects a compound-induced reduction in the number of cells in phases from S to M, whereas the induction of apoptosis involves inhibition of expression of Bcl-2 and enhanced expression of Bax with consequent reduced activation of the proapoptotic caspase 3. Finally, preliminary experiments carried out with tumor cells from myelogenous leukaemic patients showed that the compounds 4c, 4l, 4m, and 4n are indeed capable of inducing apoptosis.

引用

页码：1674 / 1687

页数：14

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