- Anthraquinonic derivatives having an antitumor activity and applications thereof
-
Said derivatives have the general formula (I) and are: STR1 (I-A) 4,6,7-trimethyl-5,8,8a,10a-tetrahydro-1H-1-azaanthracen-2,9,10-trione; (I-B) 2-ethoxy-3-methyl-1-azaanthracen-9,10-dione; (I-C) 3-ethyl-1,8-dihydro-1H-1,8-diazaanthracen-2,7,9,10-tetraone;
- -
-
-
- Tyrphostins. 5. Potent inhibitors of platelet-derived growth factor receptor tyrosine kinase: Structure-activity relationships in quinoxalines, quinolines, and indole tyrphostins
-
A series of 3-indoleacrylonitrile tyrphostins, 2-chloro-3- phenylquinolines, and 3-arylquinoxalines were prepared and tested for inhibition of platelet-derived growth factor receptor tyrosine kinase (PDGF- RTK) activity. The potency of the inhibitors was found to be quinoxalines > quinolines > indoles. Lipophilic groups (methyl, methoxy) in the 6 and 7 positions and phenyl at the 3 position of quinoxalines and quinolines were essential for potency, in contrast to the hydrophilic catechol group in tyrphostins active against EGFR kinase inhibition at different sites. The inhibitors showed selectivity for PDGF and were not active against EGF receptor and HER-2/c-ErbB-2 receptor.
- Gazit, Aviv,App, Harald,McMahon, Gerald,Chen, Jefferey,Levitzki, Alexander,Bohmer, Frank D.
-
p. 2170 - 2177
(2007/10/03)
-
- SYNTHESIS OF 2,5,8(1H)-QUINOLINETRIONE DERIVATIVES THROUGH VILSMEIER-HAACK FORMYLATION OF 2,5-DIMETHOXYANILIDES
-
The preparation of 2,5,8(1H)-quinolinetrione derivatives bearing both electron-withdrawing and electron-releasing groups at C3 is described.The reaction sequence employed involves Vilsmeier-Haack cyclization of 2,5-dimethoxyanilides into 3-substituted 5,8-dimethoxy-2-chloroquinolinolines, followed by hydrolysis to the corresponding 2(1H)-quinolinones and oxidative demethylation with cerium ammonium nitrate.
- Alonso, Miguel Angel,Blanco, M del Mar,Avendano, Carmen,Menendez, J. Carlos
-
p. 2315 - 2326
(2007/10/02)
-