Triazoles as Efficient Anticancer Agents against Colorectal Carcinoma Cells, Synthesis and Evaluation

被引:0
|
作者
Lin, Lianjun [1 ]
Yang, Yanping [1 ]
Dong, Linjuan [1 ]
机构
[1] Shaanxi Fash Engn Univ, Sch Hlth, Xian 712046, Peoples R China
来源
LATIN AMERICAN JOURNAL OF PHARMACY | 2023年 / 42卷 / 10期
关键词
click chemistry; colorectal carcinoma; synthesis tretinoin; triazoles; CANCER;
D O I
暂无
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
In the present study synthesis of tretinoin-triazoles was designed for evaluation against colorectal carcinoma cells. Results from MTT assay revealed that all the tested tretinoin triazoles significantly (p < 0.05) reduced the viability of HT29 and HCT116 cells. The cell viability was decreased to minimum %age on treatment with compound 6g at 5 mu M for 48 h. The compound 6g effectively decreased colony forming potential of HT29 and HCT116 cells compared to the control cells. Treatment of the cells with 5 mu M compound 6g led to a prominent decrease in invasion potential of tested CRC cells. Compound 6g treatment led to a prominent reduction in NRP2 protein expression after 48 h in HT29 and HCT116 cells. Moreover, a prominent decrease in expression of N-cadherin and Vimentin proteins in HT29 and HCT116 cells was observed on treatment with compound 6g. The expression of E-cadherin protein showed a prominent increase in compound 6g treated HT29 and HCT116 cells. In summary, the study identified compound 6g as the most active molecule among the synthesized library of tretinoin-triazoles. Compound 6g inhibited viability of CRC cells, suppressed invasion and colony formation potential. Moreover, it targeted NRP2, N-cadherin and Vimentin expression & up -regulated E-cadherin level in HT29 and HCT116 cells. Therefore, compound 6g has a potential to be studied further for the development of treatment for colorectal cancer.
引用
收藏
页码:2147 / 2153
页数:7
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