Abstract
A cannabinoid anticancer para-quinone, HU-331, which was synthesized by our group five decades ago, was shown to have very high efficacy against human cancer cell lines in-vitro and against in-vivo grafts of human tumors in nude mice. The main mechanism was topoisomerase IIα catalytic inhibition. Later, several groups synthesized related compounds. In the present presentation, we review the publications on compounds synthesized on the basis of HU-331, summarize their published activities and mechanisms of action and report the synthesis and action of novel quinones, thus expanding the structure-activity relationship in these series.
Original language | American English |
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Article number | 1761 |
Pages (from-to) | 1-16 |
Journal | Molecules |
Volume | 26 |
Issue number | 6 |
DOIs | |
State | Published - 2 Mar 2021 |
Bibliographical note
Funding Information:Acknowledgments: We thank to H. Ben-Bassat for providing us with human cancer cell lines. We thank Christoph Denk for assistance in preparation of the t-butyl derivative. Maximilian Peters was supported by scholarship from the Lesmüller Foundation.
Funding Information:
We thank to H. Ben-Bassat for providing us with human cancer cell lines. We thank Christoph Denk for assistance in preparation of the t-butyl derivative. Maximilian Peters was supported by scholarship from the Lesm?ller Foundation.
Publisher Copyright:
© 2021 by the authors. Licensee MDPI, Basel, Switzerland.
Keywords
- Anti-cancer
- Cannabinoid
- Quinones
- Structure-activity relationship
- cannabinoid
- quinones
- anti-cancer
- structure-activity relationship