Department of Chemistry, Bharathiar University, Coimbatore, Tamil Nadu, India.
Eur J Med Chem. 2011 Nov;46(11):5580-90. doi: 10.1016/j.ejmech.2011.09.024. Epub 2011 Sep 22.
The newly synthesized pyrido[2,3-a]carbazoles were prepared in good yields by multicomponent reactions under L-proline as promoter and structurally characterized. Few compounds showed significant activity toward both gram-positive, gram-negative bacterial strains. All compounds exerted negative efficacy for antifungal activity except compounds 5f and 7f which showed moderate activity. All compounds showed weak to moderate capacity for scavenging DPPH. The cytotoxicity was evaluated by Sulforhodamine B assay against A-549, B16F10, HCT-15, SKMel2 and SKOV3 cell lines and compared with standard drug cisplatin. Compound 5f outperformed cisplatin against A-549, HCT-15, SKMel2 and B16F10 cell lines. Compound 5e outranged cisplatin against A-549, HCT-15, and SKMel2 cell lines. 5b outperformed cisplatin specifically against B16F10. The preliminary structure activity relationships were carried out.
新合成的吡啶并[2,3-a]咔唑类化合物通过脯氨酸作为促进剂的多组分反应以良好的产率得到制备，并进行了结构表征。一些化合物对革兰氏阳性和革兰氏阴性菌均表现出显著的活性。除化合物 5f 和 7f 具有中等活性外，所有化合物对真菌均无活性。所有化合物对 DPPH 的清除能力均较弱至中等。通过 Sulforhodamine B 测定法对 A-549、B16F10、HCT-15、SKMel2 和 SKOV3 细胞系进行了细胞毒性评估，并与标准药物顺铂进行了比较。化合物 5f 在 A-549、HCT-15、SKMel2 和 B16F10 细胞系中对顺铂的活性优于顺铂。化合物 5e 在 A-549、HCT-15 和 SKMel2 细胞系中对顺铂的活性优于顺铂。化合物 5b 对 B16F10 细胞系的活性优于顺铂。进行了初步的构效关系研究。
