Related Experiment Video
Updated: Apr 5, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Novel dibenzo[b,d]furan-1H-1,2,4-triazole derivatives: Synthesis and antitumor activity
Xing Chen, Yi-Min Shi, Chao Huang
1Key Laboratory of Medicinal Chemistry for Natural Resource Yunnan University Kunming, Yunnan 650091, P. R. China. xdyang@ynu.edu.cn.
Abstract:
Twenty-four new dibenzo[b,d]furan-1H-1,2,4-triazole derivatives were synthesized and investigated for in vitro cytotoxic activity against five tumor cell lines. The results show that the substitution at 4-position of the 1,2,4-triazole with a benzyl, 4-bromophenacyl or naphthylacyl group could be crucial for prommoting cytotoxic activity. Especially, compound 28 was found to be the most powerful derivative with IC50 values lower than 3.50 μM against five investigated tumor cell lines, while compound 19 showed selective activity against leukemia (HL-60) and breast carcinoma (MCF-7) cell lines with IC50 values of 0.80 and 1.76 μM, respectively. Compound 19 can induce cell cycle arrest at G2/M phase and apoptosis in SMMC-7721 cells.
Related Concept Videos
Diazonium Group Substitution with Halogens and Cyanide: Sandmeyer and Schiemann Reactions
Aryldiazonium Salts to Azo Dyes: Diazo Coupling
Diazonium Group Substitution: –OH and –H
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase
Nucleophilic Aromatic Substitution of Aryldiazonium Salts: Aromatic SN1
In the Sandmeyer reaction, for example, the diazonio group is replaced by a chloro, bromo,...

