2. Academic Validation
  3. Synthesis and Antitumor Activity of Diosgenin Hydroxamic Acid and Quaternary Phosphonium Salt Derivatives

Synthesis and Antitumor Activity of Diosgenin Hydroxamic Acid and Quaternary Phosphonium Salt Derivatives

  • ACS Med Chem Lett. 2022 Apr 19;13(5):786-791. doi: 10.1021/acsmedchemlett.1c00581.
Lin Wang 1,  Maoling Yao 1,  Yuegao Hu 1,  Congdi Chen 2,  Liming Jin 3,  Xiaodong Ma 4,  Hongjun Yang 1
Affiliations

Affiliations

  • 1 Key Laboratory of General Chemistry of the National Ethnic Affairs Commission, School of Chemistry and Environment, Southwest Minzu University, Chengdu 610041, China.
  • 2 College of Chemistry and Life Science, Chengdu Normal University, Chengdu 611130, China.
  • 3 Key Laboratory of Biotechnology and Bioresources Utilization, Ministry of Education, Dalian Minzu University, Dalian 116600, China.
  • 4 College of Pharmacy, Dalian Medical University, Dalian 116044, China.
PMID: 35586422 DOI: 10.1021/acsmedchemlett.1c00581
Abstract

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 colon adenocarcinoma cells), H358 (human nonsmall cell lung Cancer cells), HCT116 (human colorectal adenocarcinoma cells), 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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