102729-51-1Relevant academic research and scientific papers
Quinoxalin-2-one derivatives, compositions which protect useful plants and comprise these derivatives, and processes for their preparation and their use
-
Page/Page column 34, (2008/06/13)
Compounds of the formula (I) and salts thereof in which X is O or S; (Y)n=n substituents Y, n is 0, 1, 2, 3 or 4, R1 is H, OH, NH2, (C1-C4)-alkylamino, di-[(C1-C4)-alkyl]amino or optionally substituted (C1-C10)-alkyl, (C3-C10)-alkenyl, (C3-C10)-alkynyl or (C1-C10)-alkoxy, (C3-C10)-cycloalkyl, (C4-C10)-cycloalkenyl, aryl or heterocyclyl, R2 is H or optionally substituted (C1-C10)-alkyl, (C3-C10)-alkenyl, (C3-C10)-alkynyl, (C3-C10)-cycloalkyl, (C4-C10)-cycloalkenyl, aryl or heterocyclyl, where the radicals Y are as defined in claim 1 are suitable for use as safeners for crop plants or useful plants against the phytotoxic actions of agrochemicals such as pesticides in these plants.
Quinoxaline chemistry. Part 11.3-Phenyl-2[phenoxy- and phenoxymethyl]- 6(7) or 6,8-substituted quinoxalines and n-[4-(6(7)-substituted or 6,8- disubstituted-3-phenylquinoxalin-2,yl) hydroxy or hydroxymethyl] benzoylglutamates. Synthesis and evaluation of in vitro anticancer activity and enzymatic inhibitory activity against dihydrofolate reductase and thymidylate synthase
Corona, Paola,Vitale, Gabriella,Loriga, Mario,Paglietti, Giuseppe,Costi, Maria Paola
, p. 480 - 493 (2007/10/03)
Twenty-four out of twenty-nine quinoxalines were selected at the National Cancer Institute, Bethesda, Md, USA, for in vitro anticancer screening. Among these, 10 derivatives exhibited high values of percent tumor growth inhibition at a concentration of 10-4 M in all cancer cell lines. Four of these compounds maintained these values at 10-5 M, whereas a certain number exhibited significant values of percent inhibition at the most diluted concentrations (10-8-10-6 M). Inhibitory activity against dihydrofolate reductase (DHFR) (bovine and rat liver) was determined for the most active compounds. This test showed that this type of quinoxaline exhibited an appreciable activity in comparison with the previously described aza analogues. In the other test (Lactobacillus casei, thymidylate synthase (TS), human HTS) no or poor activity was detected in both series of compounds.
Quinoxaline chemistry. Part 7. 2-[aminobenzoates]- and 2- [aminobenzoylglutamate]-quinoxalines as classical antifolate agents. Synthesis and evaluation of in vitro anticancer, anti-HIV and antifungal activity
Loriga,Piras,Sanna,Paglietti
, p. 157 - 166 (2007/10/03)
Thirty-three quinoxalines bearing an aminobenxoyl or aminobenzoylglutammate group on position 2 and various substituents on position 3,6,7 of the heterocycle were prepared in order to evaluate in vitro anticancer activity. Preliminary screening performed at NCI showed that most derivatives exhibited a moderate to strong growth inhibition activity on various tumor panel cell lines between 10-5 and 10-4 molar concentrations. Interesting selectivities were also recorded between 10-8 and 10-6. Among the series examined one compound (29) which was the most active also exhibited both in vitro anti-HIV protection and antifungal activity while in other two (31.37) the antifungal activity was prevailing.
