Tzanova Tzvetomira, Gerova Mariana, Petrov Ognyan, Karaivanova Margarita, Bagrel Denyse
Medical University of Sofia, Faculty of Pharmacy, Department of Pharmacology and Toxicology, 2 Dunav Street, Sofia 1000, Bulgaria.
Eur J Med Chem. 2009 Jun;44(6):2724-30. doi: 10.1016/j.ejmech.2008.09.010. Epub 2008 Sep 19.
Considering that oxidative stress is strongly implicated in the toxicity of chemotherapy, much effort is focused on the research of diverse antioxidants as protective agents. An efficient synthesis of three novel benzophenones containing 1,3-thiazol moiety (6a-c) is described. Their antioxidant power was evaluated in vitro and in three cell lines (the cancerous MCF7 and the non-cancerous hTERT-HME1 mammary cells, and the H9c2 cardiomyoblastic cells). One analogue 5-(2,5-dihydroxybenzoyl)-2(3H)-benzothiazolone (6c), displayed an important antioxidant activity, a low cytotoxicity, and could decrease reactive oxygen species production generated by tert-butyl hydroperoxide (tBHP) in all three cell lines. Interestingly, 6c was able to protect the non-cancerous cells against tBHP-induced death. Further studies are underway to determine its relevance as an adjuvant in oxidative stress inducing chemotherapy.
鉴于氧化应激与化疗毒性密切相关，目前大量研究致力于寻找各种抗氧化剂作为保护剂。本文描述了三种含1,3 - 噻唑部分的新型二苯甲酮（6a - c）的高效合成方法。在体外以及三种细胞系（癌性MCF7细胞、非癌性hTERT - HME1乳腺细胞和H9c2心肌母细胞）中评估了它们的抗氧化能力。其中一种类似物5 - (2,5 - 二羟基苯甲酰基)-2(3H)-苯并噻唑酮（6c）表现出重要的抗氧化活性、低细胞毒性，并且能够降低叔丁基过氧化氢（tBHP）在所有三种细胞系中产生的活性氧。有趣的是，6c能够保护非癌细胞免受tBHP诱导的死亡。目前正在进行进一步研究以确定其作为氧化应激诱导化疗辅助剂的相关性。
