DESIGN, SYNTHESIS AND ANTICANCER ACTIVITIES OF NOVEL UNSATURATED FATTY ACID-BASED beta-HYDROXY 1,2,3-TRIAZOLES

被引：2

作者：

Manneganti, Vijay ^{[1
]}

Prabhavathi Devi, Lakshmi Anu Bethala ^{[1
]}

Rachapudi, Badari Narayana Prasad ^{[1
]}

Singh, Ashita ^{[2
]}

Ummanni, Ramesh ^{[2
]}

机构：

[1] Indian Inst Chem Technol, Ctr Lipid Res, Hyderabad 500007, Andhra Pradesh, India

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

来源：

INTERNATIONAL JOURNAL OF PHARMACEUTICAL SCIENCES AND RESEARCH | 2015年 / 6卷 / 04期

关键词：

Fatty acid; Epoxidation; Azidolysis; Click reaction; beta-Hydroxy 1,2,3-Triazole; Cytotoxic activity;

D O I：

10.13040/IJPSR.0975-8232.6(4).1635-49

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

A series of novel unsaturated fatty acid based. hydroxy 1,2,3-triazole hybrids were designed and synthesised in excellent yields by esterification, epoxidation of oleic, ricinoleic and 10-undecenoic acids followed by azidolysis and "click" reaction with different alkynes. All the beta-hydroxy 1,2,3-triazole hybrids were characterised by ESI-MS, IR and NMR spectra as well as HRMS analysis and were screened in vitro for their anticancer activity against selected four human cancer cell lines (DU-145, HeLa, MCF-7 and A549) in comparison with doxorubicin, a standard anticancer drug. Among all the triazoles, methyl oleate with-CH2OH as 1,2,3-triazole side chain (1dii) exhibited good anti cancer activity against DU-145, HeLa, MCF-7 and A549 human cancer cell lines with IC50 values 10.73, 13.61, 11.93, and 16.54 mu M respectively.

引用

页码：1635 / 1649

页数：15

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