Synthesis of novel triazole/isoxazole functionalized 7-(trifluoromethyl)pyrido[2,3-d]pyrimidine derivatives as promising anticancer and antibacterial agents

被引：76

作者：

Kumar, R. Naresh ^{[1
,4
]}

Dev, G. Jitender ^{[1
,4
]}

Ravikumar, N. ^{[1
]}

Swaroop, D. Krishna ^{[1
,4
]}

Debanjan, B. ^{[2
]}

Bharath, G. ^{[3
]}

Narsaiah, B. ^{[1
,4
]}

Jain, S. Nishant ^{[2
]}

Rao, A. Gangagni ^{[3
]}

机构：

[1] CSIR, Fluoroorgan Div, Indian Inst Chem Technol, Hyderabad 500007, Andhra Pradesh, India

[2] CSIR, Med Chem & Pharmacol Div, Indian Inst Chem Technol, Hyderabad 500007, Andhra Pradesh, India

[3] CSIR, Bioengn & Environm Sci, Indian Inst Chem Technol, Hyderabad 500007, Andhra Pradesh, India

[4] CSIR, Acad Sci & Innovat Res, Indian Inst Chem Technol, Hyderabad 500007, Andhra Pradesh, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2016年 / 26卷 / 12期

关键词：

Pyrido[2,3-d]pyrimidine; Triazole; Isoxazole; Anticancer; 1,3-Dipolar cycloaddition; Sharpless conditions; CLICK CHEMISTRY; KINASE INHIBITORS; DIURETIC ACTIVITY; DISCOVERY; ANALOGS; BINDING; POTENT;

D O I：

10.1016/j.bmcl.2016.04.038

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/isoxazole functionalized pyrido[2,3-d] pyrimidine derivatives 6a-c, 7a-h and 8a-e were prepared in series of synthetic steps. All the compounds screened for the anticancer activity against four human cancer cell lines using Nocodazole as standard. Compounds 7d and 7h showed highest activity against PANC-1 (pancreatic cancer) and A549 (lung cancer) cell lines respectively and more than standard. All the compounds also screened for antibacterial activity using Rifampicin and Ciprofloxacin as standards and identified promising compounds further evaluated for minimum inhibitory concentration to validate the data. (C) 2016 Elsevier Ltd. All rights reserved.

引用

页码：2927 / 2930

页数：4

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