2. Academic Validation
  3. Synthesis and biological activity of stable and potent antitumor agents, aniline nitrogen mustards linked to 9-anilinoacridines via a urea linkage

Synthesis and biological activity of stable and potent antitumor agents, aniline nitrogen mustards linked to 9-anilinoacridines via a urea linkage

  • Bioorg Med Chem. 2008 May 15;16(10):5413-23. doi: 10.1016/j.bmc.2008.04.024.
Naval Kapuriya 1,  Kalpana Kapuriya,  Xiuguo Zhang,  Ting-Chao Chou,  Rajesh Kakadiya,  Yu-Tse Wu,  Tung-Hu Tsai,  Yu-Ting Chen,  Te-Chang Lee,  Anamik Shah,  Yogesh Naliapara,  Tsann-Long Su
Affiliations

Affiliation

  • 1 Institute of Biomedical Sciences, Laboratory of Bioorganic Chemistry, Academia Sinica, Taipei 115, Taiwan.
PMID: 18450456 DOI: 10.1016/j.bmc.2008.04.024
Abstract

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.

Figures
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z