188630-47-9Relevant academic research and scientific papers
Synthesis and evaluation of quindoline derivatives as G-quadruplex inducing and stabilizing ligands and potential inhibitors of telomerase
Zhou, Jin-Lin,Lu, Yu-Jing,Ou, Tian-Miao,Zhou, Jun-Min,Huang, Zhi-Shu,Zhu, Xiao-Feng,Du, Cui-Juan,Bu, Xian-Zhang,Ma, Lin,Gu, Lian-Quan,Li, Yue-Ming,Chan, Albert Sun-Chi
, p. 7315 - 7321 (2005)
A new series of quindoline derivatives (4a-j) were designed and synthesized to develop novel and potent telomerase inhibitors. The interaction of the G-quadruplex of human telomere DNA with these newly designed molecules was examined via circular dichroism spectroscopy and electrophoretic mobility shift assay (EMSA). The selectivity between the quindoline derivative (4a) and G-quadruplex or duplex DNA was investigated by competition dialysis. These new compounds as inhibitors of telomerase were also investigated through the utilization of modified telomerase repeat amplification protocol (TRAP) assay. The results revealed that the introduction of electron-donating groups such as substituted amino groups at the C-11 position of quindoline significantly improved the inhibitory effect on telomerase activity (TelIC 50 > 138 μM for quindoline, 0.44-12.3 μM for quindoline derivatives 4a-j). The quindoline derivatives not only stabilized the G-quadruplex structure but also induced the G-rich telomeric repeated DNA sequence to fold into quadruplex.
Synthesis and antitumor activity of fused quinoline derivatives. IV. Novel 11-aminoindolo[3,2-b]quinolines
Takeuchi, Yasuo,Oda, Toshiaki,Chang, Ming-Rong,Okamoto, Yoko,Ono, Junko,Oda, Yoko,Harada, Kyoko,Hashigaki, Kuniko,Yamato, Masatoshi
, p. 406 - 411 (2007/10/03)
Indolo[3,2-b]quinoline derivatives (1) having various amine moieties were prepared and their antitumor activities against P388 leukemia in mice were evaluated, for the purpose of gaining an insight into the role of the amine moiety in the antitumor activity and searching for an effective amine moiety. Introduction of a methylene group between the phenyl group and amino or methanesulfonamido group resulted in decrease or loss of activity.
