Synthesis and biological evaluation of novel phenanthridinyl piperazine triazoles via click chemistry as anti-proliferative agents

被引：30

作者：

Nagesh, Hunsur Nagendra ^{[1
]}

Suresh, Narva ^{[1
]}

Prakash, Gollapalli Venkata Subrahmanya Bhanu ^{[2
,3
]}

Gupta, Samarth ^{[1
]}

Rao, Janapala Venkateswara ^{[2
]}

Sekhar, Kondapalli Venkata Gowri Chandra ^{[1
]}

机构：

[1] Birla Inst Technol & Sci Pilani, Dept Chem, Hyderabad 500078, Telangana, India

[2] Indian Inst Chem Technol, Div Biol, Hyderabad 500607, Telangana, India

[3] Univ Teknol MARA UiTM, CDDR Lab, Fac Pharm, Selangor 42300, Darul Ehsan, Malaysia

来源：

MEDICINAL CHEMISTRY RESEARCH | 2015年 / 24卷 / 02期

关键词：

Phenanthridine; Piperazine; Antiproliferative activity; Click chemistry; Microwave synthesis; ANTICANCER AGENTS; DERIVATIVES;

D O I：

10.1007/s00044-014-1142-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The preliminary results describe synthesis of a series of novel 6-(4-((substituted-1H-1,2,3-triazol-4-yl)methyl)piperazin-1-yl)phenanthridine analogs using hybrid approach employing copper(I)-catalyzed azide-alkyne cycloaddition and their evaluation as antiproliferative agents against four cancer cell lines by MTT assay. Among the synthesized compounds, 7g and 7h showed good activity against all the test cell lines. In particular, 7g (IC50 = 9.73 +/- A 4.09 A mu M) exhibited excellent activity against THP1 cancer cell line, and 7h (IC50 = 7.22 +/- A 0.32 A mu M) emerged as more active compound than the standard drug etoposide against HL60 cancer cell line.

引用

页码：523 / 532

页数：10

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