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Synthesis and in-vitro cytotoxicity evaluation of gatifloxacin Mannich bases
Perumal Yogeeswari1, Dharmarajan Sriram, Ramkumar Kavya
1Medicinal Chemistry Research Laboratory, Pharmacy group, Birla Institute of Technology and Science, Pilani-333031, India. pyogee@bits-pilani.ac.in
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.
