ChemInform Abstract: Synthesis and Cytotoxic Activity of 11-Nitro and 11-Amino Derivatives of Acronycine and 6-Demethoxyacronycine.

Among 3-(2-aminopropyl)-1,2,4-thiadiazole derivatives contatining substitution-ready secondary amino group and exhibiting cytotoxic towards rat C 6 glioma cells three compounds with LD 50 values ranged from 6 to 48 мM were chosen. For these compounds amides with docosahexaenoic acid were synthetised and their cytotoxic activity was studied. It was shown that, although docosahexaenoic acid itself was not toxic for C 6 glioma cells, its addition to the amino derivatives of 1,2,4-thiadiazole increased or decreased resultant cytotoxicity. The effect depended on the structure of 1,2,4-thiadiazole substituents. The obtained data show that the acylation of cytotoxic compounds with docosahexaenoic acid does not necessarily lead to the increase of their activity, but sometimes can inactivate a compound. This fact should be taken into account, especially in the case of anti-cancer drug development.

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Synthesis, Docking Studies into CDK-2 and Anticancer Activity of New Derivatives Based Pyrimidine Scaffold and Their Derived Glycosides

Mini-Reviews in Medicinal Chemistry ◽

10.2174/1389557519666190312165717 ◽

2019 ◽

Vol 19 (13) ◽

pp. 1093-1110 ◽

Cited By ~ 5

Author(s):

Adel A.H. Abdel Rahman ◽

Ibrahim F. Nassar ◽

Amira K.F. Shaban ◽

Dina S. EL-Kady ◽

Hanem M. Awad ◽

...

Keyword(s):

Anticancer Activity ◽

Human Liver ◽

Docking Studies ◽

Cyclin Dependent Kinase ◽

Binding Interaction ◽

Enzyme Active Site ◽

Human Liver Cancer ◽

Amino Derivatives ◽

Activity Behavior ◽

Derivatives Of

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.

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Thermal cyclocondensations of 3-N(4- and 5-benzimidazolyl and benztriazolyl)amino derivatives of 2-propenoic acid

Collection of Czechoslovak Chemical Communications ◽

10.1135/cccc19872918 ◽

1987 ◽

Vol 52 (12) ◽

pp. 2918-2925 ◽

Cited By ~ 10

Author(s):

Viktor Milata ◽

Dušan Ilavský

Keyword(s):

Uv Spectra ◽

Propenoic Acid ◽

Amino Derivatives ◽

Derivatives Of ◽

C Nmr ◽

Ir And Uv Spectra

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.

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