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
相关论文
共 50 条
  • [41] Synthesis and Evaluation of Bakuchiol Derivatives as Potential Anticancer Agents
    Wu, Cheng-Zhu
    Liu, Da-Chuan
    Guo, Xing
    Dai, Yiqun
    Ma, Tao
    Li, Hong-Mei
    Huo, Qiang
    MOLECULES, 2018, 23 (03):
  • [42] Synthesis and evaluation of functionalized indoles as antimycobacterial and anticancer agents
    Cihan-Ustundag, Gokce
    Capan, Gultaze
    MOLECULAR DIVERSITY, 2012, 16 (03) : 525 - 539
  • [43] Synthesis of cinnamils and quinoxalines and their biological evaluation as anticancer agents
    Wang, Ruei-Yu
    Li, Cai-Wei
    Cho, Shu-Tse
    Chang, Chun-Hao
    Chen, Jih-Jung
    Shih, Tzenge-Lien
    ARCHIV DER PHARMAZIE, 2022, 355 (05)
  • [44] Synthesis of novel 1,2,4-triazoles and triazolo-thiadiazines as anticancer agents
    Farghaly, Thoraya Abd El-Reheem
    Abdallah, Magda Ahmad
    Mahmoud, Huda Kamel
    TURKISH JOURNAL OF CHEMISTRY, 2015, 39 (05) : 955 - 969
  • [45] Synthesis of Novel Indolyl-1,2,4-triazoles as Potent and Selective Anticancer Agents
    Kumar, Dalip
    Narayanam, Maruthi Kumar
    Chang, Kuei-Hua
    Shah, Kavita
    CHEMICAL BIOLOGY & DRUG DESIGN, 2011, 77 (03) : 182 - 188
  • [46] Synthesis and biological evaluation of novel pyrrolopyrrolizinones as anticancer agents
    Rochais, C.
    Lisowski, V.
    Dallemagne, P.
    Rault, S.
    BIOORGANIC & MEDICINAL CHEMISTRY, 2006, 14 (24) : 8162 - 8175
  • [47] Synthesis and Evaluation of Chalcone Derivatives as Novel Anticancer Agents
    Sheng, Qiwei
    Zhao, Wanqiu
    Zeng, Ming
    Xie, Zhongpao
    Xia, Yaping
    Cui, Dongmei
    CHINESE JOURNAL OF ORGANIC CHEMISTRY, 2019, 39 (03) : 703 - 708
  • [48] Synthesis of benzothiazole derivatives and their biological evaluation as anticancer agents
    Rosanna Caputo
    Maria Luisa Calabrò
    Nicola Micale
    Aaron D. Schimmer
    Moshin Ali
    Maria Zappalà
    Silvana Grasso
    Medicinal Chemistry Research, 2012, 21 : 2644 - 2651
  • [49] Synthesis and biological evaluation of new polyaromatic anticancer agents
    Bandyopadhyay, Debasish
    Short, John
    Granados, Chris
    Banik, Bimal K.
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2011, 241
  • [50] Synthesis and evaluation of nitrate derivatives of colchicine as anticancer agents
    Shen, Li Hong
    Li, Ya
    Zhang, Da Hai
    Lai, Yi Sheng
    Liu, Li Jie
    CHINESE CHEMICAL LETTERS, 2011, 22 (07) : 768 - 770