Antitumor and antimetastatic activities of a novel benzothiazole-2-thiol derivative in a murine model of breast cancer

نویسندگان

  • XiaoLin Hu
  • Sen Li
  • Yan He
  • Ping Ai
  • Shaoyong Wu
  • Yonglin Su
  • Xiaolin Li
  • Lei Cai
  • Xingchen Peng
چکیده

The prognosis of metastatic breast cancer is always very poor. Thus, it is urgent to develop novel drugs with less toxicity against metastatic breast cancer. A new drug (XC-591) derived from benzothiazole-2-thiol was designed and synthesized in our lab. In this study, we tried to assess effects of XC-591 treatment on primary breast cancer and pulmonary metastasis in 4T1 mice model. Furthermore, we tried to discover its possible molecular mechanism of action. MTT experiment showed XC-591 had significant anti-cancer activity on diverse cancer cells. Furthermore, XC-591 significantly suppressed the proliferation of 4T1 cells by colony formation assay. The in vivo results displayed that XC-591 could inhibit the growth and metastasis in 4T1 model. Moreover, histological analysis revealed that XC-591 treatment increased apoptosis, inhibited proliferation and angiogenesis in vivo. In addition, XC-591 did not contribute to obvious drug associated toxicity during the whole study. Molecular mechanism showed XC-591 could inhibit RhoGDI, activate caspase-3 and decrease phosphorylated Akt. The present data may be important to further explore this kind of new small-molecule inhibitor.

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عنوان ژورنال:

دوره 8  شماره 

صفحات  -

تاریخ انتشار 2017