title: Synthesis and in-vitro cytotoxicity evaluation of gatifloxacin Mannich bases.
abstract: Mannich bases of gatifloxacin were synthesized by reacting them with formaldehyde and several isatin derivatives. Their chemical structures have been confirmed by means of their IR, 1H-NMR data and by elemental analysis. The compounds were tested in-vitro against a panel of 58 human tumour cell lines derived from nine neoplastic diseases. Among them compound 1-cyclopropyl-6-fluoro-8-methoxy-1,4-dihydro-4-oxo-7[[N4-(3'-sulphadoximino)-1'-(5-bromoisatinyl) methyl]-3-methyl N1-piperazinyl]-3-quinoline carboxylic acid (6) emerged as a potent anticancer agent being more active than standard DNA topoisomerase II inhibitor, etoposide against 30 cancer cell lines.
authors.affiliation: Medicinal Chemistry Research Laboratory, Pharmacy group, Birla Institute of Technology and Science, Pilani-333031, India. pyogee@bits-pilani.ac.in
authors.forename: Perumal
authors.initials: P
authors.lastname: Yogeeswari
authors.forename: Dharmarajan
authors.initials: D
authors.lastname: Sriram
authors.forename: Ramkumar
authors.initials: R
authors.lastname: Kavya
authors.forename: Sonali
authors.initials: S
authors.lastname: Tiwari
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000633:toxicity*; D045744:Cell Line, Tumor; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D004354:Drug Screening Assays, Antitumor; D005047:Etoposide / Q000494:pharmacology; D005260:Female; D024841:Fluoroquinolones / Q000138:chemical synthesis* / Q000633:toxicity*; D005557:Formaldehyde / Q000737:chemistry; D000077734:Gatifloxacin; D006801:Humans; D020128:Inhibitory Concentration 50; D007510:Isatin / Q000031:analogs & derivatives* / Q000737:chemistry; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D008352:Mannich Bases / Q000138:chemical synthesis* / Q000737:chemistry; D015394:Molecular Structure; D012015:Reference Standards; D013055:Spectrophotometry, Infrared
chemical_list: D000970:Antineoplastic Agents; D024841:Fluoroquinolones; D008352:Mannich Bases; D005557:Formaldehyde; D005047:Etoposide; D007510:Isatin; D000077734:Gatifloxacin