Synthesis and biological evaluation of novel N-substituted benzamides as anti-migration agents for treatment of osteosarcoma.
Synthesis and biological evaluation of novel N-substituted benzamides as anti-migration agents for treatment of osteosarcoma.
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DOI：
10.1016/j.ejmech.2021.113203
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发表时间：
2021-01
影响因子：
6.7
通讯作者：
Xiaojing Chen;Guangbao Wang;Ali Mohammed Mohammed Alsayed-Ali-Mohammed-Mohammed-Alsayed-2124191324;Zong-Bo Du;Lu liu;Yue Ma;P. Liu;Qianwen Zhang;Xianxin Chen;Wenbin Chen;Faqing Ye;Xiaohui Zheng;Zhiguo Liu
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文献类型：
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作者：
Xiaojing Chen;Guangbao Wang;Ali Mohammed Mohammed Alsayed-Ali-Mohammed-Mohammed-Alsayed-2124191324;Zong-Bo Du;Lu liu;Yue Ma;P. Liu;Qianwen Zhang;Xianxin Chen;Wenbin Chen;Faqing Ye;Xiaohui Zheng;Zhiguo Liu
合成了一系列新型N-取代（吲哚或吲唑）苯甲酰胺，并评估了它们的抗肿瘤特性。大多数测试的化合物都具有中等的细胞毒性，但令人鼓舞的是，我们证实活性化合物通过在体外抑制骨肉瘤 (OS) 细胞的粘附、迁移和侵袭而呈现出惊人的优势。从机制上讲，我们证实5通过与粘附、迁移和侵袭相关的基因的表达抑制OS细胞的迁移能力。 5d的这种作用表明它可以作为一些侵袭性和/或转移性癌症的潜在化疗药物，以及与其他临床抗癌药物联合使用。反过来，这可以增强治疗效果或降低细胞迁移的风险。
A novel series of novelN-substituted (indole or indazole) benzamides were synthesized, and their anti-tumor properties were evaluated. The majority of tested compounds possessed moderate cytotoxicity, but inspiringly, we verified that active compound5dpresents an astonishing advantage by inhibiting the adhesion, migration, and invasion of osteosarcoma (OS) cellsin vitro. Mechanistically, we confirmed5dinhibited the migration ability of OS cells via the expression of genes related to adhesion, migration, and invasion. This effects of5dsuggest that it can be used as a potential chemotherapeutic drug to some aggressive and/or metastatic cancers, as well as in combination with other clinical anti-cancer drugs. In turn, this could enhance the therapeutic effect or reduce the risk of cell migration.