Synthesis and cytotoxicity evaluation of 1-[3-(9H-carbazol-4-yloxy)-2-hydroxypropyl]-3-aryl-1H-pyrazole-5-carboxylic acid derivatives

被引：49
|
作者：
Nagarapu, Lingaiah [1 ]
Gaikwad, Hanmant K. [1 ]
Sarikonda, Kartheeka [1 ]
Mateti, Jhansi [1 ]
Bantu, Rajashaker [1 ]
Raghu, P. S. [1 ]
Manda, Krishna Madhuri [2 ]
Kalvendi, Shasi Vardhan [2 ]
机构：
[1] Indian Inst Chem Technol, Organ Div 2, Hyderabad 500607, Andhra Pradesh, India
[2] Indian Inst Chem Technol, Ctr Chem Biol, Hyderabad 500607, Andhra Pradesh, India
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 11期
关键词：
Cytotoxicity; Neuroblastoma cell line (SK-N-SH); A549 cell line; MCF-7 cell line; Pyrazole-carbazole derivatives; Growth inhibition; AGENTS; ASSAY;
D O I：
10.1016/j.ejmech.2010.07.004
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Several novel molecules, 1-(3'-(9H-carbazol-4-yloxy)-2'-hydroxypropyl)-3-aryl-1H-pyrazole-5-carboxylic acid derivatives 3a-g were synthesized and screened to evaluate their cytotoxicity against cancer cells in vitro. The compounds 3a-g has been prepared by the reaction of ethyl 3-aryl-1H-pyrazole-5-carboxylate with 4-oxiranylmethoxy-9H-carbazole in moderate to excellent yields. The cytotoxicity of synthesized compounds was evaluated by a SRB (sulforhodamine B) assay against cancer cell such as SK-N-SH human neuroblastoma (NB), human A549 lung carcinoma, human breast cancer MCF-7 cell lines. The results showed that seven compounds can suppress SK-N-SH tumor cancer cell growth. Among them, compound 3d was the most effective small molecule in inhibiting SK-N-SH cell growth. (C) 2010 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码：4720 / 4725
页数：6
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