Design, synthesis and anticancer activity of functionalized spiro-quinolines with barbituric and thiobarbituric acids

被引：23

作者：

Bhaskarachar, Ravi Kiran ^{[1
]}

Revanasiddappa, Vijayakumar G. ^{[1
]}

Hegde, Subramanya ^{[2
]}

Balakrishna, Janardhana P. ^{[3
]}

Reddy, Suman Y. ^{[4
]}

机构：

[1] Tumkur Univ, UCS, Dept Chem, Tumakuru 572103, India

[2] Govt Sci Coll, Dept Chem, Bangalore, Karnataka, India

[3] Stellixir Biotech Pvt Ltd, Bangalore 560057, Karnataka, India

[4] Indian Inst Technol, Dept Chem, Kanpur 208016, Uttar Pradesh, India

来源：

MEDICINAL CHEMISTRY RESEARCH | 2015年 / 24卷 / 09期

关键词：

Spiro-quinoline; Barbituric acid; Benzisoxazole; 1-5] Shift; MTT assay; Flow cytometry; FREE-RADICAL SCAVENGERS; ACRIDONE ALKALOIDS; ASYMMETRIC HYDROGENATION; HYDROXAMIC ACIDS; QUINAZOLINE; DERIVATIVES; DYES; STREPTOMYCES-NITROSPOREUS-30643; LIGANDS; SYSTEMS;

D O I：

10.1007/s00044-015-1408-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of spiro-quinoline compounds have been accomplished by the reaction of barbituric acid or thiobarbituric acid with derivatives of benzisoxazole-5-carbaldehyde or 2-substituted benzaldehyde. These compounds were evaluated for their in vitro cytotoxicity on two mammalian cancer cell lines MCF-7 and KB. The compounds exhibit cytotoxicity against these cell lines in micromolar range. Among the series of compounds, 11(a-j) particularly 11b and 11e showed relatively good activity against both the tested cell lines. Compound 11b was found to exhibit the highest cytotoxic activity with IC50 value 90.2 mu M for MCF-7 and 49.8 mu M for KB cell line. Flow cytometric analysis study confirmed that these molecules induced cytotoxicity via apoptosis.

引用

页码：3516 / 3528

页数：13

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