1036724-69-2Relevant articles and documents
Synthesis and biological activity of stable and potent antitumor agents, aniline nitrogen mustards linked to 9-anilinoacridines via a urea linkage
Kapuriya, Naval,Kapuriya, Kalpana,Zhang, Xiuguo,Chou, Ting-Chao,Kakadiya, Rajesh,Wu, Yu-Tse,Tsai, Tung-Hu,Chen, Yu-Ting,Lee, Te-Chang,Shah, Anamik,Naliapara, Yogesh,Su, Tsann-Long
, p. 5413 - 5423 (2008/12/21)
To improve the chemical stability and therapeutic efficacy of N-mustard, a series of phenyl N-mustard linked to DNA-affinic 9-anilinoacridines and acridine via a urea linker were synthesized and evaluated for antitumor studies. The new N-mustard derivatives were prepared by the reaction of 4-bis(2-chloroethyl)aminophenyl isocyanate with a variety of 9-anilinoacridines or 9-aminoacridine. The antitumor studies revealed that these agents exhibited potent cytotoxicity in vitro without cross-resistance to taxol or vinblastine and showed potent antitumor therapeutic efficacy in nude mice against human tumor xenografts. It also showed that 24d was capable of inducing marked dose-dependent levels of DNA cross-linking by comet assay and has long half-life in rat plasma.