Kogan Natalya M, Peters Maximilian, Mechoulam Raphael
Institute for Drug Research, Medical Faculty, Hebrew University, Jerusalem 91120, Israel.
Molecules. 2021 Mar 21;26(6):1761. doi: 10.3390/molecules26061761.
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.
一种大麻素类抗癌对醌化合物HU-331,是我们团队在五十年前合成的,已证明其在体外对人癌细胞系以及在裸鼠体内对人肿瘤移植瘤具有非常高的疗效。其主要机制是拓扑异构酶IIα催化抑制。后来,几个研究小组合成了相关化合物。在本报告中,我们回顾了基于HU-331合成的化合物的相关文献,总结了它们已发表的活性和作用机制,并报告了新型醌类化合物的合成与作用,从而扩展了这些系列化合物的构效关系。