New (S)-verbenone-isoxazoline-1,3,4-thiadiazole hybrids: synthesis, anticancer activity and apoptosis-inducing effect.

Abstract

Background: This study aimed to develop novel isoxazoline-1,3,4-thiadiazole hybrids from (S)-verbenone for potential anticancer treatment, particularly focusing on cytotoxic and apoptotic effects in hormone-sensitive MCF-7 and triple-negative MDA-MB-231 breast cancer cells. Methods & results: (S)-verbenone was used to synthesize hybrids through 1,3-dipolar cycloaddition, followed by thorough characterization. The compounds were screened across cancer cell lines, showing significant anticancer effects. Compound 8b notably induced apoptosis via the caspase-3/7 pathway and cell cycle arrest, displaying noteworthy cytotoxicity against MCF-7 and MDA-MB-231 cells. Conclusion: These findings underscore the potential of (S)-verbenone isoxazoline-1,3,4-thiadiazole derivatives for breast cancer therapy due to their remarkable apoptotic activity. This study highlights a promising avenue for advancing breast cancer treatment using these derivatives, founded on (S)-verbenone, showcasing their distinct potential for inducing apoptosis.

• Authors: Mourad Fawzi, Abdoullah Bimoussa, Yassine Laamari, Abdellah N'ait Oussidi, Ali Oubella, El Mostafa Ketatni, Mohamed Saadi, Lahcen El Ammari, Hamid Morjani, Moulay Youssef Ait Itto, Aziz Auhmani
• Journal: Future medicinal chemistry (Future Med Chem) Vol. 15 Issue 17 Pg. 1603-1619 (09 2023) ISSN: 1756-8927 [Electronic] England
• PMID: 37772541 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• 1,3,4-thiadiazole
• verbenone
• Antineoplastic Agents

Topics

• Humans
• Female
• Cell Line, Tumor
• Antineoplastic Agents (pharmacology)
• Breast Neoplasms (drug therapy)
• Apoptosis
• Cell Proliferation
• Drug Screening Assays, Antitumor
• MCF-7 Cells