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| Autori principali: | , , , , , , , , |
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| Natura: | Artículo Open Access |
| Pubblicazione: |
Wiley
2026
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| Soggetti: | |
| Accesso online: | https://chemistry-europe.onlinelibrary.wiley.com/doi/10.1002/cmdc.70285 |
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Sommario:
- Antiproliferative Activity and Acute Toxicity of α,β‐Bis(diphenylphosphine Oxide)ethanes Obtained by Bisphosphorylation of Acetylenes: Electrosynthesis Under Mild Conditions Versus Improved Superbasic Medium Synthesis Maxim V. Tarasov Tatyana V. Gryaznova Kamil Ivshin Sergey A. Katsyuba Oksana. A. Lenina Anna P. Lyubina Andrey A. Parfenov A. D. Voloshina Yulia H. Budnikova ChemMedChem A series of vicinal bis(diphenylphosphine oxide)ethanes were synthesized via the α,β‐bisphosphorylation of aryl‐substituted acetylenes. Optimized reaction conditions were established, affording the desired compounds in moderate to good yields. The synthesized derivatives were evaluated for cytotoxic activity against a panel of cancer cell lines (M‐HeLa, MCF‐7, HuTu 80, A549), and nonmalignant cells (WI‐38 and Chang Liver). The highest efficacy was observed against the M‐HeLa cell line, with IC50 values ranging from 1.4 to 3.9 μM, which is 9–25 times more potent than the activity of sorafenib, a reference drug. Lead compounds 3g and 3d demonstrated selectivity toward M‐HeLa cells compared to Chang liver cells, suggesting their potential therapeutic value. Mechanistic investigations revealed that 3g and 3d induce dose‐dependent apoptosis via the mitochondrial pathway. Key findings indicate G2/M phase cell cycle arrest independent of the p53 pathway. Furthermore, a significant decrease in tubulin polymerization‐promoting protein (TPPP) levels was observed, indicating tubulin depolymerization and antimitotic activity. Additionally, compound 3d exhibited inhibitory activity against cyclin‐dependent kinase 2 (CDK2). These results position bis(diphenylphosphine oxide) derivatives as a promising scaffold for the development of novel anticancer agents. 10.1002/cmdc.70285 http://onlinelibrary.wiley.com/termsAndConditions#vor