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Design, synthesis, and antitumor evaluation of novel anthraquinone derivatives
Medicinal Chemistry Research ( IF 2.6 ) Pub Date : 2020-06-18 , DOI: 10.1007/s00044-020-02587-4
Larissa A. Oliveira , Heloiza D. Nicolella , Ricardo A. Furtado , Nerilson M. Lima , Denise C. Tavares , Taís A. Corrêa , Mauro V. Almeida

N-alkylated and O-alkylated anthraquinone derivatives with structures analogous to mitoxantrone were synthesized, characterized, and evaluated for their cytotoxic properties against three tumor cell lines (Human Breast Adenocarcinoma MCF-7, Human Cervical Adenocarcinoma HeLa, and Human Glioblastoma M059J) and a normal cell line (human lung fibroblasts GM-07492A). A structure-activity relationship study was carried out to verify the influence of lipophilic chain size on the biological activity of these compounds. The results indicated promising candidates for antineoplastic agents for the cancers evaluated, since these compounds showed significant selectivity and high cytotoxic potential for cancer cells, rather than mitoxantrone, the compound of which is already used in anticancer therapy.

中文翻译:

新型蒽醌衍生物的设计,合成和抗肿瘤评估

合成,表征和表征具有类似于米托蒽醌结构的N-烷基化和O-烷基化的蒽醌衍生物对三种肿瘤细胞系(人乳腺癌MCF-7,人宫颈腺癌HeLa和人胶质母细胞瘤M059J)的细胞毒性。正常细胞系(人肺成纤维细胞GM-07492A)。进行了结构活性关系研究,以验证亲脂性链大小对这些化合物的生物学活性的影响。结果表明,所评估的癌症抗肿瘤药的候选药物很有希望,因为这些化合物对癌细胞具有显着的选择性和高细胞毒性潜力,而不是米托蒽醌,后者已用于抗癌治疗。
更新日期:2020-06-18
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