二氢氟喹诺酮查尔酮衍生物的合成及抗肿瘤活性研究.pdf

3．Conclusion Inthis diethanolaminosubstituted chalcone-like article，twenty-eihgt fluoroquinolone 1H and derivativeswere and theirstructureswereconfirmedNMR synthesized，and by designed ofantitumorinvitrorevealedthatthetitle had IR data．Theresults activity compounds spectral cancercelllines．It thatitisnot effects fivetested necessary varyinginhibitoryagainst suggests theC-7 to anti-tumor fortheC一3 acid and develop carboxylicgroup piperazinylgroup lead couldbe and replacedbymethylenegroup fluoroquinolonecompounds，they diethanolamino group，respectively． KEY activity． IV 目录 摘要…………………………………………………。 ABSTRACT………………………．………．．．……………………………………．．．……………．………．．．……．．．．III 第一章序言………………………………．．．………………………………………………………………………1 1．1研究背景………………………………………………………………………………．．1 1．2喹诺酮类药物的作用机制…-…………………………………………………………3 1．2．1抗菌作用机制………………………………………………………………………3 1．2．2抗肿瘤作用机制……………………………………………………………………3 1．3喹诺酮药物的构效关系及其抗肿瘤活性…………．…………………………………．3 1．3．1 N．1位结构修饰及其抗肿瘤活性变化……………………………………………．4 1．3．2 C．2位的结构修饰及抗肿瘤活性变化……………………………………………．4 1．3．3 C．3和C-4位的结构修饰及抗肿瘤活性变化……………………………………．5 1．3．4 C．5位的结构修饰及抗肿瘤活性变化……………………………………………．7 1．3．5 C．6位的结构修饰及抗肿瘤活性变化……………………………………………．7 1．3．6 C．7位的结构修饰及抗肿瘤活性变化……………………………………………．8 1．3．7 C一8位的结构修饰及抗肿瘤活性变化……………………………………………．9 1．3．8