Synthesis and Biological Evaluation of Novel 2-imino-4-thiazolidinones as
Potential Antitumor Agents for Glioblastoma
作者:José Coan Campos、Patrick Teixeira Campos、Nathalia Pontes Bona、Mayara Sandrielly Soares、Priscila Oliveira Souza、Elizandra Braganhol、Wilson Cunico、Geonir Machado Siqueira
DOI:10.2174/1573406417666210806094543
日期:2022.5
synthesize and characterize a series of novel 2-imino-4-thiazolidinones and evaluate their antiglioblastoma activity. METHODS The 2-imino-4-thiazolidinone (5a-p) was synthesized according to the literature with modifications. Compounds were identified and characterized using spectroscopic analysis and X-ray diffraction. The antitumor activity was analyzed by 3-(4,5- dimethyl)-2,5-diphenyltetrazolium bromide
目的 我们研究的目的是探索2-亚氨基-4-噻唑烷酮和吡啶支架之间的分子杂交及其潜在的抗肿瘤活性。背景胶质母细胞瘤是临床诊断为恶性且高度复发的原发性脑肿瘤类型中最具侵袭性的胶质瘤。胶质母细胞瘤的治疗标准是手术,然后使用替莫唑胺进行放疗和化疗。然而,化疗耐药已成为治疗成功的主要障碍。2-亚氨基-4-噻唑烷酮是一类重要的杂环化合物,具有抗癌活性;然而,抗胶质母细胞瘤的活性仍有待探索。目的合成和表征一系列新型2-亚氨基-4-噻唑烷酮类药物并评价其抗胶质母细胞瘤活性。方法 2-亚氨基-4-噻唑烷酮(5a-p)是根据文献经过修改合成的。使用光谱分析和 X 射线衍射鉴定和表征化合物。通过 3-(4,5-二甲基)-2,5-二苯基溴化四唑 (MTT) 测定法在原代星形胶质细胞和胶质瘤 (C6) 中分析抗肿瘤活性。通过流式细胞术分析确定细胞凋亡和细胞周期阶段。用发光法测定caspase-3/7的表达。氧化应激