Design and synthesis of novel 1,2,3-triazole derivatives of coronopilin as anti-cancer compounds

被引：36

作者：

Khazir, Jabeena ^{[2
]}

Hyder, Irfan ^{[1
]}

Gayatri, J. Laxmi ^{[1
]}

Yandrati, Leela Prasad ^{[1
]}

Nalla, Naresh ^{[1
]}

Chasoo, Gousia ^{[2
]}

Mahajan, Ajay ^{[2
]}

Saxena, A. K. ^{[2
]}

Alam, M. S. ^{[3
]}

Qazi, G. N. ^{[3
]}

Kumar, Halmuthur M. Sampath ^{[1
]}

机构：

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

[2] CSIR Indian Inst Integrat Med, Div Med Chem, Jammu 180001, India

[3] Jamia Hamdard, Dept Chem, New Delhi 110062, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 82卷

关键词：

Sesquiterpenoid lactone; Parthenin; Coronopilin; 1,2,3-Triazole; NF-kappa B (p65) inhibitors; NF-KAPPA-B; PARTHENIN; APOPTOSIS;

D O I：

10.1016/j.ejmech.2014.05.053

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 1,2,3-triazole coronopilin congeners have been designed and synthesized by employing click chemistry approach starting from parthenin and evaluated for their cytotoxicity against a panel of six human cancer cell lines (PC-3, THP-1, HCT-15, HeLa, A-549 and MCF-7). While many compounds exhibited significant anticancer activity, compound 3a, was found to be the most promising analogue in this series with IC50 values of 3.1 mu M on PC-3 cell line. Flow-cytometric studies showed that 1,2,3-triazole derivative-3a induce dose dependent apoptosis in the sub G1 phase. This lead molecule-3a was further studied for NF-kappa B (p65) transcription factor inhibitory activity using Elisa and western blotting analysis which confirmed concentration dependent inhibitory activity against NF-kappa B, p65 with 80% inhibition in 24 h at 100 mu M. (C) 2014 Elsevier Masson SAS. All rights reserved.

引用

页码：255 / 262

页数：8

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