120651-07-2Relevant academic research and scientific papers
Synthesis, cytotoxic characterization, and SAR study of imidazo[1,2-b]pyrazole-7-carboxamides
Demjén, András,Alf?ldi, Róbert,Angyal, Anikó,Gyuris, Márió,Hackler, László,Szebeni, Gábor J.,W?lfling, János,Puskás, László G.,Kanizsai, Iván
, (2018/07/13)
The synthesis and in vitro cytotoxic characteristics of new imidazo[1,2-b]pyrazole-7-carboxamides were investigated. Following a hit-to-lead optimization exploiting 2D and 3D cultures of MCF-7 human breast, 4T1 mammary gland, and HL-60 human promyelocytic leukemia cancer cell lines, a 67-membered library was constructed and the structure–activity relationship (SAR) was determined. Seven synthesized analogues exhibited sub-micromolar activities, from which compound 63 exerted the most significant potency with a remarkable HL-60 sensitivity (IC50 = 0.183 μM).
α-Dimethylaminomethylenation-induced Houben-Hoesch-type cyclization of cyanoacetanilides: A practical synthesis of 3-formyl-4-hydroxyquinolin-2(1H)- ones
Kobayashi, Yusuke,Nakatani, Terue,Tanaka, Rie,Okada, Mari,Torii, Eri,Harayama, Takashi,Kimachi, Tetsutaro
experimental part, p. 3457 - 3463 (2011/06/17)
The tandem reaction of cyanoacetanilides with triflic anhydride in DMF proceeded at room temperature to afford 3-formyl-4-hydroxyquinolin-2(1H)-ones in good to high yields. A detailed mechanistic study revealed that the tandem reaction proceeded via α-dim
Reactions of diethyl 2-(ethoxymethylene)malonate with 2-cyanoacetanilides: Unexpected transfer of the ethoxymethylene moiety
Tkachova, Valeriya P.,Gorobets, Nikolay Yu.,Tkachov, Roman P.,Dyachenko, Oleksandr D.,Rusanov, Eduard B.,Dyachenko, Vladimir D.
scheme or table, p. 254 - 264 (2011/02/27)
A sodium ethoxide catalyzed reaction of N-substituted cyanoacetanilides 1a-f with diethyl 2-(ethoxymethylene)malonate 2 unexpectedly leads to the corresponding 2-amino-5-cyano-6-oxo-N,1-diaryl-1,6-dihydropyridine-3- carboxamides 3a-f, while the expected 5
ACETALS OF LACTAMS AND AMIDES. 42. REACTIONS OF ENAMINO AMIDES AND ENAMINO ESTERS WITH SOME FORMYLATING AGENTS. SYNTHESIS OF DERIVATIVES OF 2-PYRIDONE AND OF PYRIMIDIN-4- AND -6-ONES
Granik, V. G.,Ershov, L. V.,Grizik, S. I.,Chistyakov, V. V.
, p. 1026 - 1031 (2007/10/02)
The reactions of enamino esters and enamino amides with the diethyl acetal of dimethylformamide and with orthoformic ester have been investigated and it has been shown that the process takes place in two directions - with the formation of pyrimidone or 2-
Substituted phenyl-5-aminopyrazoles
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, (2008/06/13)
This disclosure describes novel substituted phenyl-5-aminopyrazoles useful as anxiolytic and/or anti-depressant agents.
