Das Arnika, Kumar Sujeet, Persoons Leentje, Daelemans Dirk, Schols Dominique, Alici Hakan, Tahtaci Hakan, Karki Subhas S
Department of Pharmaceutical Chemistry, KLE College of Pharmacy, Bengaluru, 560010, Karnataka, India.
Dr Prabhakar B Kore Basic Science Research Centre, Off-Campus, KLE College of Pharmacy, A Constituent Unit of KLE Academy of Higher Education and Research-Belagavi, Bengaluru, 560010, Karnataka, India.
Heliyon. 2021 Jan 30;7(1):e05893. doi: 10.1016/j.heliyon.2020.e05893. eCollection 2021 Jan.
Series of ()1-benzyl-4-((4-styrylphenoxy)methyl)-1-1,2,3-triazoles were obtained by Wittig reaction between 4-((1-benzyl-1-1,2,3-triazol-4-yl)methoxy)benzaldehydes and benzyl triphenylphosphonium halides in benzene. The structures of the synthesized compounds were confirmed by FTIR, NMR (H and C NMR) spectroscopy, and mass spectrometry. All synthesized compounds were screened for their cytotoxic activity against human cancer cell lines including pancreatic carcinoma, colorectal carcinoma, lung carcinoma, and leukemias such as acute lymphoblastic, chronic myeloid, and non-Hodgkinson lymphoma cell lines. cytotoxicity data showed that compounds , , , , , , and were moderately cytotoxic (11.6-19.3 μM) against the selected cancer cell lines. These cytotoxicity findings were supported using molecular docking studies of the compounds against 1TUB receptor. The drug-likeness properties of the compounds evaluated by ADME analyses. Resveratrol linked 1,2,3-triazoles were more sensitive towards human carcinoma cell lines but least sensitive towards leukemia and lymphoma cell lines.
通过4-((1-苄基-1,2,3-三唑-4-基)甲氧基)苯甲醛与苄基三苯基卤化鏻在苯中进行维蒂希反应，得到了一系列( )1-苄基-4-((4-苯乙烯基苯氧基)甲基)-1,2,3-三唑。通过傅里叶变换红外光谱(FTIR)、核磁共振(NMR)(氢谱和碳谱)光谱以及质谱对合成化合物的结构进行了确证。对所有合成化合物针对包括胰腺癌、结直肠癌、肺癌以及白血病（如急性淋巴细胞白血病、慢性髓性白血病和非霍奇金淋巴瘤细胞系）等人类癌细胞系的细胞毒性活性进行了筛选。细胞毒性数据表明，化合物 、 、 、 、 、 和 对所选癌细胞系具有中等细胞毒性(11.6 - 19.3 μM)。使用这些化合物针对1TUB受体的分子对接研究对这些细胞毒性研究结果进行了支持。通过ADME分析评估了这些化合物的类药性质。白藜芦醇连接的1,2,3-三唑对人类癌细胞系更敏感，但对白血病和淋巴瘤细胞系最不敏感。
