Synthesis, antitumor activity and in silico analyses of amino acid derivatives of artepillin C, drupanin and baccharin from green propolis

2021 ◽  
Vol 47 ◽  
pp. 116372
Author(s):  
Débora Munhoz Rodrigues ◽  
Gisele Bulhões Portapilla ◽  
Guilherme Martins Silva ◽  
Andressa Duarte ◽  
Cristiana Gonçalez Rotta ◽  
...  
Keyword(s):  
Amino Acid ◽  
Antitumor Activity ◽  
In Silico ◽  
Amino Acid Derivatives ◽  
Artepillin C ◽  
Derivatives Of ◽  
In Silico Analyses

scholarly journals Research in vivo the qualities of potential antitumor amino-acid derivatives of glycosides of indolocarbazol

2017 ◽  
Vol 16 (4) ◽  
pp. 85-92 ◽  
Author(s):  
I. S. Golubeva ◽  
N. P. Yavorskaya ◽  
O. V. Goryunova
Keyword(s):  
Amino Acid ◽  
Antitumor Activity ◽  
Optimal Dose ◽  
Amino Acid Derivatives ◽  
Tumor Growth Inhibition ◽  
Active Metabolites ◽  
Derivatives Of ◽  
Potential Antitumor

Background. The addition of active metabolites (in particular, amino acids) to the molecule affects the physicochemical and prodrug properties of derivatives of indolocarbazoles. Using computed chemoinformatics, probability antitumor activity of amino-acid derivatives of glycosides of indolocarbazol (AADGI) is predicted with low probability of their cytotoxic activity in vitro. Based on these data, a study of these compounds in vivo is conducted. Objective: the assessment of AADGI as potential antitumor medications. Materials and methods. Research antitumor activity of AADGI was done using murine tumor models - cervical cancer CC-5. Investigated compounds were injected to mice СВА abdominally 5-times daily with interval of 24 h. Observation of animals were continued till their death. Antitumor effect of compounds was assessed by criteria of tumor growth inhibition and increase in life expectancy of mice comparing to control animals. Results. The optimal dose for these series of compounds was titrated and this dose is 100 mg/kg. Antitumor activity of AADGI was assessed on CC-5. Conclusions. Based on data received we suggest an extended study in vivo of antitumor qualities of selected 5 leader AADGI.

scholarly journals In silico and in vitro research of potential antineoplastic amino acid derivatives of indolocarbazol glycosides properties

2017 ◽  
Vol 16 (4) ◽  
pp. 46-54 ◽  
Author(s):  
G. N. Apryshko ◽  
O. S. Zhukova ◽  
L. V. Fetisova ◽  
N. K. Vlasenkova ◽  
R. B. Pugacheva ◽  
...  
Keyword(s):  
Amino Acid ◽  
Antitumor Activity ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Molecular Descriptors ◽  
Human Tumor ◽  
Amino Acid Derivatives ◽  
Computer Methods ◽  
Derivatives Of

Objective: to evaluate the prospects of the glycosides of indolocarbazole containing amino acid residues as potential antitumor compounds. Materials and methods. For 32 compounds by structural formulas using the methods of chemoinformatics, a number of molecular descriptors and the probability of manifestation of various types of biological activity were calculated, the cytotoxic activity was evaluated in vitro by methylthiazole tetrazolium (MTT) assay using five human tumor cell lines. Results. For the studied amino acid derivatives of glycosides of indolocarbazole, a high probability of antitumor activity with a low probability of cytotoxic activity in vitro is predicted by computer method. Low cytotoxic activity was confirmed in the MTT test on 5 cell lines. Computer methods were used to predict the mechanisms of possible antitumor activity and to calculate a number of molecular descriptors that are important for the qualification of substances as potential drugs. Conclusion. It is expedient to study the antitumor activity of amino-acid derivatives of glycosides of indolocarbazole in experiments on animals with transplanted tumors.

Three Amino Acid Derivatives of Valproic Acid: Design, Synthesis, Theoretical and Experimental Evaluation as Anticancer Agents

2014 ◽  
Vol 14 (7) ◽  
pp. 984-993 ◽  
Author(s):  
Gabriela Luna-Palencia ◽  
Federico Martinez-Ramos ◽  
Ismael Vasquez-Moctezuma ◽  
Manuel Fragoso-Vazquez ◽  
Jessica Mendieta-Wejebe ◽  
...  
Keyword(s):  
Valproic Acid ◽  
Amino Acid ◽  
Anticancer Agents ◽  
Experimental Evaluation ◽  
Amino Acid Derivatives ◽  
Design Synthesis ◽  
Derivatives Of

scholarly journals Novel Amino Acid Derivatives of Quinolines as Potential Antibacterial and Fluorophore Agents

2020 ◽  
Vol 88 (4) ◽  
pp. 57
Author(s):  
Oussama Moussaoui ◽  
Rajendra Bhadane ◽  
Riham Sghyar ◽  
El Mestafa El Hadrami ◽  
Soukaina El Amrani ◽  
...  
Keyword(s):  
Amino Acid ◽  
Methyl Esters ◽  
Amino Acid Derivatives ◽  
Bacterial Strains ◽  
Fluorescent Properties ◽  
Topoisomerase Iv ◽  
Microdilution Method ◽  
Hydrolysis Of ◽  
Derivatives Of

A new series of amino acid derivatives of quinolines was synthesized through the hydrolysis of amino acid methyl esters of quinoline carboxamides with alkali hydroxide. The compounds were purified on silica gel by column chromatography and further characterized by TLC, NMR and ESI-TOF mass spectrometry. All compounds were screened for in vitro antimicrobial activity against different bacterial strains using the microdilution method. Most of the synthesized amino acid-quinolines show more potent or equipotent inhibitory action against the tested bacteria than their correspond esters. In addition, many of them exhibit fluorescent properties and could possibly be utilized as fluorophores. Molecular docking and simulation studies of the compounds at putative bacterial target enzymes suggest that the antimicrobial potency of these synthesized analogues could be due to enzyme inhibition via their favorable binding at the fluoroquinolone binding site at the GyrA subunit of DNA gyrase and/or the ParC subunit of topoisomerase-IV.

Synthesis of Some Amino Acid Derivatives of Styrene1

1959 ◽  
Vol 81 (2) ◽  
pp. 377-382 ◽  
Author(s):  
L. R. Morris ◽  
R. A. Mock ◽  
C. A. Marshall ◽  
J. H. Howe
Keyword(s):  
Amino Acid ◽  
Amino Acid Derivatives ◽  
Derivatives Of

Synthesis of amino acid derivatives of indole-3-acetic acid

2005 ◽  
Vol 2005 (10) ◽  
pp. 640-642 ◽  
Author(s):  
Ying Liu ◽  
Liang Zhao ◽  
Liang Liu ◽  
Lin-Yi Wei ◽  
Lu-Hua Lai
Keyword(s):  
Acetic Acid ◽  
Amino Acid ◽  
Amino Acid Derivatives ◽  
H Nmr ◽  
Derivatives Of ◽  
Indole 3 Acetic Acid

Amino acid derivatives of a modified indole-3-acetic acid have been synthesised. Fourteen new dipeptide-like compounds 3–4 were obtained and their structures were elucidated based on the IR, 1H NMR, MS spectra.

Synthesis of amino acid derivatives of benzofuroxan

2013 ◽  
Vol 450 (2) ◽  
pp. 149-151 ◽  
Author(s):  
I. V. Serkov ◽  
E. A. Chugunova ◽  
A. R. Burilov ◽  
S. O. Bachurin
Keyword(s):  
Amino Acid ◽  
Amino Acid Derivatives ◽  
Derivatives Of
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