Synthesis and antitumor activity of bis(hydroxymethyl)propionate analogs of pterostilbene in cisplatin-resistant human oral cancer cells

Min Tsang Hsieh, Li Jiau Huang, Tian Shung Wu, Hui Yi Lin, Susan L. Morris-Natschke, Kuo Hsiung Lee, Sheng Chu Kuo

研究成果: Article同行評審

8 引文 斯高帕斯(Scopus)

摘要

The aim of this study was to develop a new drug substance with low toxicity and effective inhibitory activity against cisplatin-resistant oral cancer. The naturally produced pterostilbene was selected as the lead compound for design and synthesis of a series of bis(hydroxymethyl)propionate-based prodrugs. All derivatives were screened for antiproliferative effects against the cisplatin-resistant oral squamous (CAR) cell line and the results indicated that several compounds demonstrated superior inhibitory activity compared with pterostilbene and resveratrol. Among them, the most promising compound, 12, was evaluated for in vivo antitumor activity in a CAR xenograft nude mouse model. Obvious antitumor activity was observed at the lowest oral dose (25 mg/kg/day). Increasing the dose of 12 to 100 mg/kg/day reduced the tumor size to 22% of the control group. Based on these findings as well as the extremely low toxicity seen in the in vivo studies, we believe that compound 12 could serve as a new lead for further development.

原文English
頁(從 - 到)3909-3916
頁數8
期刊Bioorganic and Medicinal Chemistry
26
發行號14
DOIs
出版狀態Published - 2018 8月 7

All Science Journal Classification (ASJC) codes

  • 生物化學
  • 分子醫學
  • 分子生物學
  • 藥學科學
  • 藥物發現
  • 臨床生物化學
  • 有機化學

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