Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 13, Issue 5, Pages 786-791Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.1c00581
Keywords
Diosgenin; antitumor; derivatives; quaternary phosphonium salt; hydroxamic acid
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Funding
- National Science Fundation of China [21602183]
- Fundamental Research Funds for the Central Universities, Southwest Minzu University [2021PTJS25]
- Open Fund of Key Laboratory of Biotechnology and Bioresources Utilization (Dalian Minzu University) , Ministry of Education [KF2021005]
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In this study, two series of diosgenin derivatives were synthesized and evaluated for their cellular anticancer activities. The representative compound 2.2f exhibited significantly higher antiproliferative activities against four cell lines compared with the lead compound diosgenin.
Diosgenin, a component separated from Dioscorea plants, is an important starting material for steroid hormone drugs and semisynthetic steroids. In the work, two series of diosgenin derivatives were designed, synthesized, and evaluated for their cellular anticancer activities. Most of the target compounds exhibited good inhibitory activities against four cell lines, Aspc-1 (human and SW620 (human metastatic pancreatic cancer cells). Among them, the representative compound 2.2f exhibited 7.9-341.7-fold antiproliferative activities against the above-mentioned four cell lines compared with the lead compound diosgenin.
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