Rational design, synthesis and anti-proliferative evaluation of novel 1,4-benzoxazine-[1,2,3]triazole hybrids

被引：54

作者：

Bollu, Rajitha ^{[1
]}

Palem, Jyothsna Devi ^{[1
]}

Bantu, Rajashaker ^{[1
]}

Guguloth, Vijayacharan ^{[1
]}

Nagarapu, Lingaiah ^{[1
]}

Polepalli, Sowjanya ^{[2
]}

Jain, Nishant ^{[2
]}

机构：

[1] Indian Inst Chem Technol, CSIR, Organ Chem Div CPC 2, Hyderabad 500007, Andhra Pradesh, India

[2] Indian Inst Chem Technol, CSIR, Ctr Chem Biol, Hyderabad 500007, Andhra Pradesh, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2015年 / 89卷

关键词：

1,2,3-Triazoles; 1,4-Benzoxazine; Anti-proliferative; Apoptosis; Cell lines; POTENTIAL ANTICANCER AGENTS; CLICK CHEMISTRY; DERIVATIVES; CANCER; 1,2,3-TRIAZOLES; INHIBITORS; SCAFFOLD; ANALOGS;

D O I：

10.1016/j.ejmech.2014.10.051

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel 1,2,3-triazole-1,4-benzoxazine hybrids 5a-n were efficiently synthesized employing click chemistry approach and evaluated for anti-proliferative activity against four cancer cell lines such as HeLa (cervical), MIAPACA (pancreatic), MDA-MB-231 (breast) and IMR32 (neuroblastoma). Compounds 5n and 5g exhibited promising anti-proliferative activity with GI(50) values ranging from 1.2 to 2.5 mu M and 0.1-1.1 mu M respectively against all cell lines, like HeLa, MDA-MB-231, MIAPACA and IMR32, while compound 51 showed significant activity against MDA-MB-231 and IMR32 with GI(50) values ranging from 1.1 and 1.4 mu M. This is the first report on the synthesis and in vitro anti-proliferative evaluation of 1,2,3-triazole-1,4-benzoxazine hybrids. (C) 2014 Elsevier Masson SAS. All rights reserved.

引用

页码：138 / 146

页数：9

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