1036724-75-0Relevant academic research and scientific papers
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.
ANILINE OR PHENOL MUSTARDS LINKED TO DNA-AFFINIC MOLECULES OR WATER-SOLUBLE AROMATIC RINGS AND THEIR USE AS CANCER THERAPEUTIC AGENTS
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Page/Page column 16, (2008/12/06)
New aniline or phenol N-mustards linked to DNA-affinity carriers (such as 9-anilinoacridines, acridines andquinolines), aminobenzamides or aminophenol ethers by a urea, carbamic acid, carbanic acid ester, hydxazine urea, hydrazine carbamic acid ester, phenoxyurea, phenoxycarbamic acid ester linkage with improved chemical stability and anti-tumor therapeutic efficacy are provided.
