Yogeeswari Perumal, Sriram Dharmarajan, Kavya Ramkumar, Tiwari Sonali
Medicinal Chemistry Research Laboratory, Pharmacy group, Birla Institute of Technology and Science, Pilani-333031, India.
Biomed Pharmacother. 2005 Oct;59(9):501-10. doi: 10.1016/j.biopha.2005.06.006. Epub 2005 Sep 21.
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.
加替沙星的曼尼希碱是通过使其与甲醛和几种异吲哚酮衍生物反应合成的。它们的化学结构已通过红外光谱、¹H - NMR数据和元素分析得以证实。这些化合物针对源自9种肿瘤疾病的58种人类肿瘤细胞系进行了体外测试。其中，化合物1 - 环丙基 - 6 - 氟 - 8 - 甲氧基 - 1,4 - 二氢 - 4 - 氧代 - 7[[N⁴ - (3'-磺胺多辛亚氨基)-1'-(5 - 溴异吲哚酮基)甲基]-3 - 甲基 - N¹ - 哌嗪基]-3 - 喹啉羧酸（6）表现为一种强效抗癌剂，在针对30种癌细胞系的测试中比标准DNA拓扑异构酶II抑制剂依托泊苷更具活性。
