Reduction of nitroindazoles: Preparation of new amino and chloroamino derivatives
The synthesis of chloroaminoindazoles by the reduction of the nitro group of indazoles using stannous chloride in alcoholic acid solution is reported. Using catalytic hydrogenation with palladium the expected reduction to amino-indazoles occur.{A figure is presented}. Indazole Nitro Reduction Chlorination Aminochloroindazole Heterocycle.
Synthesis and biological evaluation of N-(7-indazolyl)benzenesulfonamide derivatives as potent cell cycle inhibitors
We herein describe a new synthesis of N-(7-indazolyl)benzenesulfonamide derivatives. These compounds were evaluated for their antiproliferative activities toward L1210 murine leukemia cells. One of them, 4-methoxy-N-(3- chloro-7-indazolyl)benzenesulfonamide, was identified as the most potent with an IC50 of 0.44 μM.
New and efficient synthesis of bi- and trisubstituted indazoles
In this paper, the synthesis of bi- and trisubstituted indazoles was described. 4-Alkoxy-7-aminoprotected-indazole or 7-aminoprotected-indazole derivatives were prepared selectively using SnCl2 in alcohol or SnCl2 in ethyl acetate, r
Bouissane, Latifa,El Kazzouli, Sa?d,Léger, Jean-Michel,Jarry, Christian,Rakib, El Mostapha,Khouili, Mostafa,Guillaumet, Gérald
p. 8218 - 8225
(2007/10/03)
Structure-activity relationships for pyrido-, imidazo-, pyrazolo-, pyrazino-, and pyrrolophenazinecarboxamides as topoisomerase-targeted anticancer agents
Heterocyclic phenazinecarboxamides were prepared by condensation of aminoheterocycles and 2-halo-3-nitrobenzoic acids, followed by reductive ring closure and amidation. They showed similar inhibition of paired cell lines that underexpressed topo II or overexpressed P-glycoprotein, indicating a non topo II mechanism of cytotoxicity and indifference to P-glycoprotein mediated multidrug resistance. Compounds with a fused five-membered heterocyclic ring were generally less potent than the pyrido[4,3-a]phenazines. A 4-methoxypyrido[4,3-a]phenazine (IC50s 2.5-26 nM) gave modest (ca. 5 day) growth delays in H69/P xenografts with oral dosing.
Gamage, Swarna A.,Spicer, Julie A.,Rewcastle, Gordon W.,Milton, John,Sohal, Sukhjit,Dangerfield, Wendy,Mistry, Prakash,Vicker, Nigel,Charlton, Peter A.,Denny, William A.
p. 740 - 743
(2007/10/03)
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