92429-91-9Relevant academic research and scientific papers
The synthesis and biological evaluation of new DNA-directed alkylating agents, phenyl N-mustard-4-anilinoquinoline conjugates containing a urea linker
Marvania, Bhavin,Kakadiya, Rajesh,Christian, Wilson,Chen, Tai-Lin,Wu, Ming-Hsi,Suman, Sharda,Tala, Kiran,Lee, Te-Chang,Shah, Anamik,Su, Tsann-Long
, p. 695 - 708 (2014/07/22)
We synthesized a series of phenyl N-mustard-4-anilinoquinoline conjugates to study their antitumorigenic effects. These agents were prepared by the condensation of 4-[N,N-bis(2-chloroethyl)amino]phenyl isocyanate with 6-amino-4-methylamino or 4-anilinoquinolines. The structure-activity relationship (SAR) studies revealed that the C2-methylquinoline derivatives (18a-o) were generally more cytotoxic than the C2-phenylquinoline conjugates (23a-d) in inhibiting the cell growth of various human tumor cell lines in vitro. However, the methylamino or aniline substituents at C4 of quinoline did not influence the cytotoxic effects. The title conjugates were capable of inducing DNA cross-linking and promoting cell-cycle arrest at the G2/M phase. This study demonstrates that phenyl N-mustard-4-anilinoquinoline conjugates are generally more potent than phenyl N-mustard-4-anilinoquinazoline conjugates against the cell growth of various tumor cell-lines.
Quinoline derivatives as immunostimulants
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, (2008/06/13)
This invention relates to compounds of the formula STR1 wherein R1, R2, R3, R4, R5, R6 and R7 are as defined hereinbelow that exhibit activity as immunostimulants.
