Fatahala Samar S, Mohamed Mosaad S, Youns Mahmoud, Abd-El Hameed Rania H
Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Helwan University, Ain-Helwan, Helwan, Cairo. Egypt.
Biochemistry and Molecular Biology Department, Faculty of Pharmacy, Helwan University, Ain-Helwan, Helwan,Cairo. Egypt.
Anticancer Agents Med Chem. 2017;17(7):1014-1025. doi: 10.2174/1871520617666170102152928.
Pyrrole derivatives represent a very interesting class as biologically active compounds. The objective of our study was to investigate the cytotoxic and apoptotic effects and antioxidant activity of the newly synthesized pyrrole derivatives.
A series of novel pyrroles and fused pyrroles (tetrahydroindoles, pyrrolopyrimidines, pyrrolopyridines and pyrrolotriazines) were synthesized and characterized using IR, 1H NMR, 13C NMR, MS and elemental analysis techniques. The antiproliferative activity of our synthesized compounds and their modulatory effect apoptotic pathway were investigated. The effect on cellular proliferation and viability was monitored by resazurin assay. Apoptotic effect was evaluated by caspase glo 3/7 assay. Synthesized compounds are then tested for their anticancer activities against three different cell lines representing three different tumor types, namely; the HepG-2 (Human hepatocellular liver carcinoma cell line), the human MCF-7 cell line (breast cancer) and the pancreatic resistant Panc-1 cells.
Compounds Ia-e, IIe, and IXc, d showed a promising anti-cancer activity on all tested cell lines. Antioxidant and wound healing invasion assays were examined for promising anticancer candidate compounds.
吡咯衍生物作为生物活性化合物是一类非常有趣的物质。我们研究的目的是探究新合成的吡咯衍生物的细胞毒性、凋亡作用及抗氧化活性。
合成了一系列新型吡咯及稠合吡咯（四氢吲哚、吡咯并嘧啶、吡咯并吡啶和吡咯并三嗪），并采用红外光谱、¹H核磁共振、¹³C核磁共振、质谱和元素分析技术对其进行表征。研究了我们合成的化合物的抗增殖活性及其对凋亡途径的调节作用。通过刃天青测定法监测对细胞增殖和活力的影响。通过胱天蛋白酶glo 3/7测定法评估凋亡作用。然后测试合成的化合物对代表三种不同肿瘤类型的三种不同细胞系的抗癌活性，即：HepG-2（人肝癌细胞系）、人MCF-7细胞系（乳腺癌）和胰腺抗性Panc-1细胞。
化合物Ia-e、IIe和IXc、d对所有测试细胞系均显示出有前景的抗癌活性。对有前景的抗癌候选化合物进行了抗氧化和伤口愈合侵袭试验。
