Synthesis and antiproliferative assay of 1,3,4-oxadiazole and 1,2,4-triazole derivatives in cancer cells.

Abstract

A series of new 1,3,4-oxadiazole and 1,2,4-triazole derivatives were synthesized. The structures were confirmed by IR, (1)H-NMR, and MS. The compounds were evaluated for their antiproliferative activity against K562 (human erythromyeloblastoid leukemia cell line), MDA-MB-231 (human breast adenocarcinoma cell line), HT29 (human colon adenocarcinoma grade II cell line) and HepG2 (human hepatocellular liver carcinoma cell line) in vitro. The result showed that 7 compounds displayed inhibitory activities against K562 with the inhibition rate more than 50%. Especially, compound 5f exhibited the most potent activity against K562 with 85% inhibition ratio and could be used as lead compound to search new 1,3,4-oxadiazole derivatives as antiproliferative agent.

• Authors: Guogang Tu, Yugang Yan, Xueying Chen, Qiaoli Lv, Jiaqi Wang, Shaohua Li
• Journal: Drug discoveries & therapeutics (Drug Discov Ther) Vol. 7 Issue 2 Pg. 58-65 (Apr 2013) ISSN: 1881-7831 [Print] Japan
• PMID: 23715503 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Oxadiazoles
• Triazoles
• 1,3,4-oxadiazole
• 1,2,4-triazole

Topics

• Antineoplastic Agents (chemical synthesis, pharmacology)
• Cell Line, Tumor
• Cell Proliferation (drug effects)
• Drug Screening Assays, Antitumor
• HT29 Cells
• Hep G2 Cells
• Humans
• K562 Cells
• Oxadiazoles (chemical synthesis, pharmacology)
• Structure-Activity Relationship
• Triazoles (chemical synthesis, pharmacology)