C5-curcuminoid-4-aminoquinoline based molecular hybrids: design, synthesis and mechanistic investigation of anticancer activity

被引：25

作者：

Kandi, Shamseer Kulangara ^{[1
]}

Manohar, Sunny ^{[1
]}

Gerena, Christian E. Velez ^{[2
]}

Zayas, Beatriz ^{[2
]}

Malhotra, Sanjay V. ^{[3
]}

Rawat, Diwan S. ^{[1
]}

机构：

[1] Univ Delhi, Dept Chem, Delhi 110007, India

[2] Univ Metropolitana, Sch Environm Affairs, San Juan, PR 00928 USA

[3] Leidos Biomed Res Inc, Frederick Natl Lab Canc Res, Lab Synthet Chem, Frederick, MD 21702 USA

来源：

NEW JOURNAL OF CHEMISTRY | 2015年 / 39卷 / 01期

基金：

美国国家卫生研究院;

关键词：

CELL-CYCLE ARREST; IMPROVED IN-VITRO; ALKYLATING-AGENTS; ANTIMALARIAL ACTIVITY; CANCER-CHEMOTHERAPY; CURCUMIN ANALOGS; APOPTOSIS; BIOAVAILABILITY; INDUCTION; CASPASE-8;

D O I：

10.1039/c4nj00936c

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

The privileged scaffolds of curcumin and 4-aminoquinolines are extensively used in the design and synthesis of biodynamic agents having remarkable efficacy against diseases like cancer and malaria. Therefore, we anticipated that covalent hybridization of these two pharmacophores via the triazole linker may lead to molecules with better anticancer activity. The synthesized hybrid compounds were tested for their anti-cancer activity on 60 human cancer cell lines, which represent diverse histologies. Our study has identified a set of these hybrids that showed excellent growth inhibition at nano-molar concentrations. The mechanistic investigations through a series of assays showed apoptotic induction as a cause for their displayed anticancer activity.

引用

页码：224 / 234

页数：11

共 56 条

[1] Synthesis and biological evaluation of novel curcumin analogs as anti-cancer and anti-angiogenesis agents [J].