Synthesis of P-Stereogenic Diarylphosphinamides as Novel Inhibitors of Melanoma

• 来源期刊: 高等学校化学研究（英文版）
• 年，卷（期）: 2019,（5）
• 页码范围: 812-816
• 页数: 5页
• 语种: 英文
• DOI: 10.1007/s40242-019-9103-8

摘要

In this paper,the evaluation on the biological activity of an array ofP-stereogenic diaryphosphinamides as novel inhibitors of malignant melanoma was presented.Among 20 derivatives being screened,several of them displayed high inhibition rate up to 90％ against the B16 melanoma cells at 100 μg/mL.Moreover,one of them displayed high inhibition activity with IC50 value of 5.8 μtg/mL.In contrast,a comparative assay showed that all the compounds were almost inactive or showed only very weak inhibition ability against an array of cell lines including HL7702,Be17402,HT1080,A549 and McF7 cells.The results suggested that the P-stereogenic diarylphosphinamides may serve as a class of novel lead molecules for further development of new inhibitors for selective inhibition of melanoma.