151. Synthesis and anticancer activities of 3-arylflavone-8-acetic acid derivatives.
- Author
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Yan GH, Li XF, Ge BC, Shi XD, Chen YF, Yang XM, Xu JP, Liu SW, Zhao PL, Zhou ZZ, Zhou CQ, and Chen WH
- Subjects
- Antineoplastic Agents chemical synthesis, Antineoplastic Agents chemistry, Cell Proliferation drug effects, Cells, Cultured, Dose-Response Relationship, Drug, Drug Screening Assays, Antitumor, Flavones chemical synthesis, Flavones chemistry, HT29 Cells, Humans, Molecular Structure, Structure-Activity Relationship, Antineoplastic Agents pharmacology, Flavones pharmacology, Leukocytes, Mononuclear drug effects
- Abstract
This paper describes the synthesis and the antiproliferative activities of compounds 9a-r, 3-aryl analogs of flavone-8-acetic acid that bear diverse substituents on the benzene rings at the 2- and 3-positions of the flavone nucleus. Their direct and indirect cytotoxicities were evaluated against HT-29 human colon adenocarcinoma cell lines, A549 lung adenocarcinoma cell lines and Human Peripheral Blood Mononuclear Cells (HPBMCs). The results indicate that most of the compounds bearing electron-withdrawing substituents (9b-m) exhibited moderate direct cytotoxicities. And compounds 9e and 9i showed comparable indirect cytotoxicities with 5, 6-dimethylxanthenone-4-acetic acid (DMXAA), and low direct cytotoxicities toward HPBMCs. Interestingly, the compounds 9n-r bearing methoxy groups at the 2- or 3-position of the flavone nucleus exhibited higher indirect cytotoxicities against A549 cell lines than DMXAA, and lower cytotoxicities against HPBMCs. In addition, compounds 9p-r were found to be able to induce tumor necrosis factor α (TNF-α) production in HPBMCs., (Copyright © 2014 Elsevier Masson SAS. All rights reserved.) more...
- Published
- 2015
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