首页|新型1H-吡咯[2,3-c]并吡啶衍生物的合成和抗胰腺癌活性评价

新型1H-吡咯[2,3-c]并吡啶衍生物的合成和抗胰腺癌活性评价

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胰腺癌恶性程度高、治疗药物少,开发具有抗胰腺癌活性的化合物有重要研究意义.通过改造1H-吡咯[2,3-c]并吡啶的氮1位,合成了 22个化合物,对所有化合物的抗胰腺癌活性进行了评价,Ⅱ-1活性表现较为突出(半抑制浓度IC50=3.61 μmol/L).利用细胞划痕实验及侵袭实验对Ⅱ-1的抗迁移能力及侵袭能力进行了研究.经1、5、10 μmol/L的Ⅱ-1处理24 h时,与对照组相比胰腺癌细胞(PANC-1细胞)迁移率分别下降28%、41%、54%;经1、5、10 μmol/L的Ⅱ-1处理48 h时,与对照组相比PANC-1迁移率分别下降25%、46%、49%;经1、5、10 μmol/L的Ⅱ-1处理48 h时,与对照组相比PANC-1细胞相对侵袭能力分别下降64%、79%、89%.实验结果表明:Ⅱ-1对PANC-1细胞具有较高的抑制活性,Ⅱ-1抑制PANC-1细胞迁移及侵袭能力也较为突出.
Synthesis and Evaluation of Anti-pancreatic Cancer Activity of Novel 1H-Pyrrolo[2,3-c]pyridine Derivatives
Pancreatic cancer has a high malignancy rate and there are very few therapeutic drugs.It is of great significance to develop compounds with anti-pancreatic cancer activity.By modifying the nitrogen at 1 position of 1H-pyrrolo[2,3-c]pyridine,22 compounds were synthesized.Compounds anti PANC-1 cell's activities were evaluated,Ⅱ-1 exhibited great activity(IC50=3.61 μmol/L).Anti migration and invasion abilities of Ⅱ-1 were studied using wound healing and invasion assay.After being treated with Ⅱ-1 at a concentration rate of 1,5,and 10 µmol/L for 24 h,the migration rates of PANC-1 cells declined 28% ,41% ,and 54% vs the control group,respectively.After being treated with Ⅱ-1 at a concentration rate of 1,5,and 10 μmol/L for 48 h,the migration rates declined 25% ,46% ,and 49% vs the control group,respectively.After being treated with Ⅱ-1 at concentration of 1,5,and 10 µmol/L for 48 h,the relative invasion abilities of PANC-1 cells declined 64% ,79% ,and 89% vs the control group,respectively.These experimental results indicate that Ⅱ-1 has high inhibitory effects on PANC-1 cells,and has prominent ability to inhibit the migration and invasion of PANC-1 cells.

chemical synthesis1H-pyrrolo[2,3-c]pyridineanti pancreatic cancer activity

曹阳、李前、崔文慧、王亚玲、司鑫鑫

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南京大学化学化工学院,江苏南京 210093

江苏德源药业股份有限公司,江苏连云港 222047

江苏海洋大学江苏省海洋药物活性分子筛选重点实验室,江苏连云港 222005

化学合成 1H-吡咯[2,3-c]并吡啶 抗胰腺癌活性

中国博士后科学基金

2023M741444

2024

精细化工中间体
湖南化工研究院

精细化工中间体

CSTPCD
影响因子:0.236
ISSN:1009-9212
年,卷(期):2024.54(3)