Synthesis and cytotoxic activity of 3-[2-(1H-Indol-3-yl)-1,3-thiazol-4-yl]-1H-pyrrolo[3,2-c]pyridine hydrobromides, analogues of the marine alkaloid nortopsentin
A new series of thiazole nortopsentin analogues with a 5-azaindole moiety was conveniently synthesized in good to excellent yields by an Hantzsch reaction between thioamides and α-bromoacetyl compounds. The cytotoxic activity of the new derivatives was tested against different human tumor cell lines of the NCI full panel. All tested compounds were active against all of the investigated cell lines showing GI50 values from micro to submicromolar levels. Some of the new analogues exhibited good selectivities against different NCI sub-panels.
Pecoraro, Camilla,Carbone, Daniela,Aiello, Daniele,Carbone, Anna
p. 30 - 42
(2021/11/27)
Site-selective azaindole arylation at the azine and azole rings via N-oxide activation
Subjection of N-methyl 6-and 7-azaindole N-oxides to a Pd(OAc) 2/DavePhos catalyst system enables regioselective direct arylation of the azine ring. Following deoxygenation, 7-azaindole substrates undergo an additional regioselective azole direct arylation event in good yield.
Huestis, Malcolm P.,Fagnou, Keith
supporting information; experimental part
p. 1357 - 1360
(2009/09/05)
4-Substituted-1-methyl-1H-pyrrolopyridines
The synthesis of a series of 4-substituted 1-methyl-1H-pyrrolopyridines is described based on transformations of 4-methyl and 4-chloro analogues.Reactivities of the latter compounds proved less than those of corresponding α-substituted pyridines, but pressure methods allowed isolation of the 4-amino and other amine derivatives in good yield.Under Mannich conditions both 4-methyl and 4-chloro derivatives were converted to bis methanes.
Casy, Alan F.,Needle, Richard J.,Upton, Christopher
p. 343 - 360
(2007/10/02)
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