Synthesis of P-Stereogenic Diarylphosphinamides as Novel Inhibitors of Melanoma

doi:10.1007/s40242-019-9103-8

高等学校化学研究 ›› 2019, Vol. 35 ›› Issue (5): 812-816.doi: 10.1007/s40242-019-9103-8

Synthesis of P-Stereogenic Diarylphosphinamides as Novel Inhibitors of Melanoma

TANG Xu¹, DU Zhijun², WU Guojie^1,2, HAN Fushe²

1. Technical Innovation Center for Utilization of Marine Biological Resources, Third Institute of Oceanography, Ministry of Natural Resources, Xiamen 361005, P. R. China;
2. Jilin Province Key Lab of Green Chemistry and Process, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, P. R. China

收稿日期:2019-04-10 出版日期:2019-10-01 发布日期:2019-09-24
通讯作者: HAN Fushe E-mail:fshan@ciac.ac.cn
基金资助:
Supported by the National Natural Science Foundation of China(No.21572215), the National Basic Research Program of China(No.2015CB75590) and the Fund of the Engineering Research Center of Marine Bioresources Comprehensive Utilization of the State Oceanic Adminstration of China.

Synthesis of P-Stereogenic Diarylphosphinamides as Novel Inhibitors of Melanoma

TANG Xu¹, DU Zhijun², WU Guojie^1,2, HAN Fushe²

1. Technical Innovation Center for Utilization of Marine Biological Resources, Third Institute of Oceanography, Ministry of Natural Resources, Xiamen 361005, P. R. China;
2. Jilin Province Key Lab of Green Chemistry and Process, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, P. R. China

Received:2019-04-10 Online:2019-10-01 Published:2019-09-24
Contact: HAN Fushe E-mail:fshan@ciac.ac.cn
Supported by:
Supported by the National Natural Science Foundation of China(No.21572215), the National Basic Research Program of China(No.2015CB75590) and the Fund of the Engineering Research Center of Marine Bioresources Comprehensive Utilization of the State Oceanic Adminstration of China.

摘要/Abstract

摘要： In this paper, the evaluation on the biological activity of an array of P-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 μg/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, Bel7402, 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.

关键词: Phosphinamide, Melanoma, Cytotoxicity, Anticancer activity, Phosphorus compound

Abstract: In this paper, the evaluation on the biological activity of an array of P-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 μg/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, Bel7402, 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.

Key words: Phosphinamide, Melanoma, Cytotoxicity, Anticancer activity, Phosphorus compound

TANG Xu, DU Zhijun, WU Guojie, HAN Fushe. Synthesis of P-Stereogenic Diarylphosphinamides as Novel Inhibitors of Melanoma[J]. 高等学校化学研究, 2019, 35(5): 812-816.

TANG Xu, DU Zhijun, WU Guojie, HAN Fushe. Synthesis of P-Stereogenic Diarylphosphinamides as Novel Inhibitors of Melanoma[J]. Chemical Research in Chinese Universities, 2019, 35(5): 812-816.

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Synthesis of P-Stereogenic Diarylphosphinamides as Novel Inhibitors of Melanoma

Synthesis of P-Stereogenic Diarylphosphinamides as Novel Inhibitors of Melanoma

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