新型奥氮平衍生物的环保合成及其抗癌潜力评估。
Eco-friendly synthesis of new olanzapine derivatives and evaluation of their anticancer potential.
作者信息
Drabczyk Anna K, Kułaga Damian, Zaręba Przemysław, Tylińska Wiktoria, Bachowski Wojciech, Archała Aneta, Wnorowski Artur, Tzani Andromachi, Detsi Anastasia, Jaśkowska Jolanta
机构信息
Faculty of Chemical Engineering and Technology, Department of Chemical Technology and Environmental Analytics, Cracow University of Technology 24 Warszawska Street 31-155 Cracow Poland
Faculty of Chemical Engineering and Technology, Department of Organic Chemistry and Technology, Cracow University of Technology 24 Warszawska Street 31-155 Cracow Poland.
出版信息
RSC Adv. 2023 Jul 10;13(30):20467-20476. doi: 10.1039/d3ra03926a. eCollection 2023 Jul 7.
New derivatives of the known antipsychotic drug olanzapine have been obtained as potential compounds with anticancer activity in two metabolically different breast cancer cell lines: MCF-7 and triple negative MDA-MB-231. The compounds were obtained under phase transfer catalysis (PTC) in the presence of microwave irradiation (MW) or ultrasound (")))"), evaluating the effect of solvents such as dimethylformamide, water, or choline chloride/urea (natural deep eutectic solvent, NaDES). In the best option, the compounds were obtained within 2 minutes with a yield of 57-86% in MW. Two of the obtained compounds which have a naphthalimide moiety and a pentyl (7) or hexyl chain (8) show pronounced cytotoxicity. Interestingly, neither olanzapine nor desmethylolanzapine (DOLA), which was one of the substrates for the synthesis reaction, showed any significant activity in the study.
已知抗精神病药物奥氮平的新衍生物已被制备出来，作为在两种代谢不同的乳腺癌细胞系（MCF-7和三阴性MDA-MB-231）中具有抗癌活性的潜在化合物。这些化合物是在相转移催化（PTC）条件下，于微波辐射（MW）或超声（“)))”）存在的情况下制备的，同时评估了二甲基甲酰胺、水或氯化胆碱/尿素（天然低共熔溶剂，NaDES）等溶剂的影响。在最佳条件下，化合物在2分钟内即可制得，微波辐射条件下产率为57 - 86%。所制备的两种含有萘二甲酰亚胺部分和戊基（7）或己基链（8）的化合物表现出显著的细胞毒性。有趣的是，合成反应的底物之一奥氮平和去甲基奥氮平（DOLA）在该研究中均未表现出任何显著活性。
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