scholarly journals Synthesis and properties of esters and amides of pyridine- and 1,2-azolcarbonic acids

Author(s):  
D. V. Kazak ◽  
Е. А. Dikusar ◽  
E. A. Akishina ◽  
R. S. Alexeev ◽  
N. A. Bumagin ◽  
...  

Based on esters of nicotinic and isonicotinic acids with hydroxybenzaldehydes, a series of functionally substituted derivatives containing isoxazole and isothiazole heterocycles in the molecule have been synthesized. Azomethines were obtained by condensation of nicotinates and isonicotinates with p-bromoaniline and m-aminophenol, which have been reduced with sodium triacetoxyborohydride to give the corresponding amines. Acylation of amino derivatives of nicotinates and isonicotinates with 5-arylisoxazole- and 4,5-dichloroisothiazolecarbonyl chlorides leads to the esters and amides with isoxazole and isothiazole residues.

2019 ◽  
Vol 19 (13) ◽  
pp. 1093-1110 ◽  
Author(s):  
Adel A.H. Abdel Rahman ◽  
Ibrahim F. Nassar ◽  
Amira K.F. Shaban ◽  
Dina S. EL-Kady ◽  
Hanem M. Awad ◽  
...  

Background & Objective:New diaryl-substituted pyrimidinedione compounds, their thioxo derivatives as well as their bicyclic thiazole compounds were synthesized and characterized.Methods:The glycosylamino derivatives of the synthesized disubstituted derivatives of the pyrimidine scaffold were also prepared via reaction of the N3-amino derivatives with a number of monosaccharides followed by acetylation.Results:The anticancer activity of the synthesized compounds was studied against human liver cancer (HepG2) and RPE-1cell lines. Compounds 2a, 2b, 3a and 12 showed potent activities with IC50 results comparable to that of doxorubicin.Conclusion:Docking investigations into Cyclin-dependent kinase 2 (CDK-2) enzyme, a potential target for cancer medication, were also reported showing the possible binding interaction into the enzyme active site to support their activity behavior.


1987 ◽  
Vol 52 (12) ◽  
pp. 2918-2925 ◽  
Author(s):  
Viktor Milata ◽  
Dušan Ilavský

The cyclization of 3-N(4- and 5-benzimidazolyl and benztriazolyl)amino-2-cyano- and 2-ethoxycarbonyl-2-propenoate esters Ia, b-IVa, b under the conditions of the Gould-Jacobs reaction leads to angularly ring-fused substituted imidazo or triazolo[4,5-f] (V, VI) and [4,5-h] (VII, VIII) quinolines, respectively. The esters Vb-VIIIb have been transformed into the corresponding chloroderivatives Vc-VIIIc. 3-N(5-Benzimidazolyl and 5-benztriazolyl)amino-2-cyano-2-propenenitriles are cyclized in the presence of aluminium(III) chloride to give the aminoquinolines Vd, VId. The structure of the products has been characterized by their 1H, 13C NMR, IR, and UV spectra.


1985 ◽  
Vol 16 (15) ◽  
Author(s):  
N. I. TRAVEN' ◽  
YU. A. ERSHOVA ◽  
A. S. SOKOLOVA ◽  
V. A. CHERNOV ◽  
T. S. SAFONOVA

2007 ◽  
Vol 2007 (25) ◽  
pp. 4257-4266 ◽  
Author(s):  
Victor P. Krasnov ◽  
Alexey Yu. Vigorov ◽  
Irina A. Nizova ◽  
Tatyana V. Matveeva ◽  
Alexander N. Grishakov ◽  
...  

1996 ◽  
Vol 32 (1) ◽  
pp. 19-22
Author(s):  
M. B. Izbosarov ◽  
B. Kh. Abduazimov ◽  
M. É. Tuichieva ◽  
M. N. Yusupov ◽  
V. M. Malikov ◽  
...  

1989 ◽  
Vol 42 (11) ◽  
pp. 1673-1683 ◽  
Author(s):  
H. A. KIRST ◽  
K. E. WILLARD ◽  
M. DEBONO ◽  
J. E. TOTH ◽  
B. A. TRUEDELL ◽  
...  

1993 ◽  
Vol 176 (1) ◽  
pp. 195-213 ◽  
Author(s):  
G. Verbeek ◽  
S. Depaemelaere ◽  
M. Van der Auweraer ◽  
F.C. De Schryver ◽  
A. Vaes ◽  
...  

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