Antioxidative and antiproliferative activities of novel pyrido[1,2-a]benzimidazoles

详细信息    查看全文

• 作者：Martina Tireli ; Kristina Starčević ; Tamara Martinović…
• 关键词：Pyrido[1 ; 2 ; a]benzimidazoles ; Amides ; Antiproliferative activity ; Antioxidative activity ; Cyclization
• 刊名：Molecular Diversity
• 出版年：2017
• 出版时间：February 2017
• 年：2017
• 卷：21
• 期：1
• 页码：201-210
• 全文大小：
• 刊物类别：Chemistry and Materials Science
• 刊物主题：Biochemistry, general; Organic Chemistry; Polymer Sciences; Pharmacy;
• 出版者：Springer International Publishing
• ISSN：1573-501X
• 卷排序：21

文摘

A series of pyrido[1,2-a]benzimidazoles has been designed, and novel examples are synthesized and evaluated for their potential antiproliferative activity against four human tumour cell lines—cervical (HeLa), colorectal (SW620), breast (MCF-7) and hepatocellular carcinoma (HepG2). In addition, their antioxidative potency has been evaluated by in vitro spectrophotometric assays. Preliminary structure–activity relationships among the synthesized compounds are discussed. Evaluation of their antioxidative capacity has shown that two compounds (25 and 26) possess promising reducing characteristics and free radical scavenging activity. Selective antiproliferative effect in the single-digit micromolar range was observed for compound 25 on MCF-7 \((\hbox {IC}_{50} = 6\,{\upmu }\hbox {M})\) and HeLa \((\hbox {IC}_{50} = 8\,{\upmu }\hbox {M})\) cell lines, comparable to the standards 5-fluorouracil and cisplatin. The combination of the radical scavenging activity and antiproliferative activity of compound 25 positions this compound as a potential lead candidate for further optimization.