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Assessment of a bifendate derivative bearing a 6,7-dihydro-dibenzo[c,e]azepine scaffold as a potential anti-metastatic agent.


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 that 4i 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 of 4i 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 compound 4i could be a promising lead for the development of novel anti-cancer agents with anti-MDR and metastatic activities.

SUBMITTER: Qiu J 

PROVIDER: S-EPMC6247821 | biostudies-other | 2018 Nov

REPOSITORIES: biostudies-other

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Assessment of a bifendate derivative bearing a 6,7-dihydro-dibenzo[<i>c</i>,<i>e</i>]azepine scaffold as a potential anti-metastatic agent.

Qiu Jingying J   Chen Wang W   Jiang Yanfei Y   Chen Jing J   Zhang Yinpeng Y   Gu Xiaoke X  

MedChemComm 20180917 11


Multidrug resistance (MDR) and metastasis are major causes of mortality in patients with cancer. We recently reported a bifendate derivative bearing a dibenzo[<i>c</i>,<i>e</i>]azepine scaffold (<b>4i</b>) 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 that <b>4i</b> could significantly attenuate the mig  ...[more]

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