title: Novel bis(indolyl)hydrazide-hydrazones as potent cytotoxic agents.
abstract: A series of bis(indolyl) hydrazide-hydrazones 5a-n were synthesized and evaluated for their cytotoxicity against selected human cancer cell lines. The reaction of indole-3-carboxaldehyde 2 with indole-3-carbohydrazide 4 in presence of catalytic amount of acetic acid afforded 5a-n in good yields. Among the synthesized bis(indolyl)hydrazide-hydrazones, the compound 5b with N-(p-chlorobenzyl) and bromo substituents was found to be the most potent against multiple cancer cell lines (IC(50)=1.0 μM, MDA-MB-231). The compound 5k exhibited selective cytotoxicity against breast cancer cell line MCF7 (IC(50)=3.1 μM).
authors: Department of Chemistry, Birla Institute of Technology and Science, Pilani 333 031, India. dalipk@bits-pilani.ac.in
authors: Dalip
authors: D
authors: Kumar
authors: N
authors: N
authors: Maruthi Kumar
authors: Soumitra
authors: S
authors: Ghosh
authors: Kavita
authors: K
authors: Shah
mesh_terms: D019342:Acetic Acid / Q000737:chemistry; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D002384:Catalysis; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D006801:Humans; D006834:Hydrazines / Q000737:chemistry* / Q000494:pharmacology; D006835:Hydrazones / Q000737:chemistry* / Q000494:pharmacology; D007211:Indoles / Q000737:chemistry*; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D009369:Neoplasms / Q000188:drug therapy*; D011161:Porifera
chemical_list: D000970:Antineoplastic Agents; D006834:Hydrazines; D006835:Hydrazones; D007211:Indoles; D019342:Acetic Acid