1. Synthesis and Preliminary Anticancer Evaluation of 4-C Derivatives of Diphyllin.
- Author
-
Zhao R, Ni X, Dong C, Xu J, and Zhao Y
- Subjects
- Humans, Cell Line, Tumor, Structure-Activity Relationship, Drug Screening Assays, Antitumor, Vacuolar Proton-Translocating ATPases antagonists & inhibitors, Vacuolar Proton-Translocating ATPases metabolism, Triazoles chemistry, Triazoles pharmacology, Triazoles chemical synthesis, Lignans pharmacology, Lignans chemistry, Lignans chemical synthesis, Antineoplastic Agents pharmacology, Antineoplastic Agents chemical synthesis, Antineoplastic Agents chemistry
- Abstract
The natural lignan diphyllin has shown promising antitumor activity, although its clinical advancement has been impeded by challenges such as low solubility, poor metabolic stability, and limited potency. In response, we developed and synthesized two sets of diphyllin 4-C derivatives, comprising six ester derivatives and eight 1, 2, 3-triazole derivatives. Notably, among these derivatives, 1, 2, 3-triazole derivatives 7c and 7e demonstrated the most potent cytotoxic effects, with IC
50 values ranging from 0.003 to 0.01 μM. Treatment with 0.2 μM of 7c and 7e resulted in a reduction of V-ATPase activity in HGC-27 cells to 23% and 29%, respectively., (© 2024 John Wiley & Sons Ltd.)- Published
- 2024
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