title: L-Proline anchored multicomponent synthesis of novel pyrido[2,3-a]carbazoles; investigation of in vitro antimicrobial, antioxidant, cytotoxicity and structure activity relationship studies.
abstract: 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.
authors: Department of Chemistry, Bharathiar University, Coimbatore, Tamil Nadu, India.
authors: T
authors: T
authors: Indumathi
authors: V S
authors: VS
authors: Jamal Ahamed
authors: Surk-Sik
authors: SS
authors: Moon
authors: Frank R
authors: FR
authors: Fronczek
authors: K J
authors: KJ
authors: Rajendra Prasad
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects; D002227:Carbazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D060326:Chemistry Techniques, Synthetic / Q000379:methods*; D015195:Drug Design; D016166:Free Radical Scavengers / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D005658:Fungi / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D008968:Molecular Conformation; D011392:Proline / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D000890:Anti-Infective Agents; D000970:Antineoplastic Agents; D002227:Carbazoles; D016166:Free Radical Scavengers; D011392:Proline