Assessment of a bifendate derivative bearing a 6, 7-dihydro-dibenzo[c, e]azepine scaffold as a potential anti-metastatic agent. Issue 11 (25th September 2018)

• Record Type: Journal Article
• Authors: Qiu, Jingying; Chen, Wang; Jiang, Yanfei; Chen, Jing; Zhang, Yinpeng; Gu, Xiaoke
• Is Part Of: MedChemComm. Volume 9:Issue 11(2018)
• Page Start: 1826
• Page End: 1830
• Publication Date: 2018-09-25
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19
• DOI: 10.1039/c8md00294k
• Languages: English
• ISSNs: 2040-2503

Abstract

Abstract : 4i exhibited significant anti-metastatic activity in MDA-MB-231 cells via inhibiting MMP-2/9 activity and expression. Abstract : Multidrug resistance (MDR) and metastasis are major causes of mortality in patients with cancer. We recently reported a bifendate derivative bearing a dibenzo[ c, e ]azepine scaffold (4i ) as a P-gp and BCRP-medicated MDR reversal agent. As a continuation of the previous research, its ability to inhibit cancer metastasis was investigated in MDA-MB-231 cells in the present work. Wound-healing and chamber migration assays showed that4i could significantly attenuate the migration of MDA-MB-231 cells. Additionally, 4i obviously suppressed the invasive activity of MDA-MB-231 cells, thus displaying potential anti-metastasis activity. Preliminary mechanism studies indicated that the anti-metastasis activity of4i was associated with the inhibitory effect on the activity and expression of MMP-2 and MMP-9. These results, together with the previous findings, suggest that compound4i could be a promising lead for the development of novel anti-cancer agents with anti-MDR and metastatic activities.