Synthesis and in vitro cytotoxicity evaluation of baicalein amino acid derivatives

2014 ◽  
Vol 11 (3) ◽  
pp. 284-288 ◽  
Author(s):  
Lei LI ◽  
Wen-Yuan LIU ◽  
Feng FENG ◽  
Chun-Yong WU ◽  
Ning XIE
Keyword(s):  
Amino Acid ◽  
In Vitro Cytotoxicity ◽  
Amino Acid Derivatives

Synthesis and in vitro cytotoxicity evaluation of some N-substituted α-amino acid derivatives containing a hexahydropyrimidine moiety

2017 ◽  
Vol 26 (5) ◽  
pp. 900-908 ◽  
Author(s):  
Dilara R. Latypova ◽  
Alexander G. Badamshin ◽  
Natalya N. Gibadullina ◽  
Nailya S. Khusnutdinova ◽  
Liana F. Zainullina ◽  
...  
Keyword(s):  
Amino Acid ◽  
In Vitro Cytotoxicity ◽  
Amino Acid Derivatives

Synthesis and in vitro cytotoxicity evaluation of baicalein amino acid derivatives

2013 ◽  
Vol 11 (3) ◽  
pp. 284-288 ◽  
Author(s):  
Lei LI ◽  
Wen-Yuan LIU ◽  
Feng FENG ◽  
Chun-Yong WU ◽  
Ning XIE
Keyword(s):  
Amino Acid ◽  
In Vitro Cytotoxicity ◽  
Amino Acid Derivatives

scholarly journals In vitro anticancer potentiality and molecular modelling study of novel amino acid derivatives based on N1,N3-bis-(1-hydrazinyl-1-oxopropan-2-yl) isophthalamide

2019 ◽  
Vol 34 (1) ◽  
pp. 1247-1258 ◽  
Author(s):  
Asmaa F. Kassem ◽  
Gaber O. Moustafa ◽  
Eman S. Nossier ◽  
Hemat S. Khalaf ◽  
Marwa M. Mounier ◽  
...  
Keyword(s):  
Amino Acid ◽  
Molecular Modelling ◽  
Amino Acid Derivatives ◽  
Modelling Study

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.

Preparation and in vitro cytotoxicity of oxaliplatin derivatives with chiral amino acid as the carrier group

2014 ◽  
Vol 67 (13) ◽  
pp. 2195-2203 ◽  
Author(s):  
Chuanzhu Gao ◽  
Tianshuai Wang ◽  
Ji Chen ◽  
Yan Zhang ◽  
Bo Yang ◽  
...  
Keyword(s):  
Amino Acid ◽  
In Vitro Cytotoxicity

In vitro studies on the inhibition of colon cancer by amino acid derivatives of bromothiazole

2017 ◽  
Vol 27 (15) ◽  
pp. 3507-3510 ◽  
Author(s):  
Nuno Vale ◽  
Ana Correia-Branco ◽  
Bárbara Patrício ◽  
Diana Duarte ◽  
Fátima Martel
Keyword(s):  
Colon Cancer ◽  
Amino Acid ◽  
In Vitro Studies ◽  
Amino Acid Derivatives ◽  
Derivatives Of

In vitro cytotoxicity of L-amino acid oxidase from the venom of Crotalus mitchellii pyrrhus

Toxicon ◽  
2017 ◽  
Vol 139 ◽  
pp. 20-30 ◽  
Author(s):  
Kok Keong Tan ◽  
Siok Ghee Ler ◽  
Jayantha Gunaratne ◽  
Boon Huat Bay ◽  
Gopalakrishnakone Ponnampalam
Keyword(s):  
Amino Acid ◽  
In Vitro Cytotoxicity ◽  
Acid Oxidase ◽  
Amino Acid Oxidase ◽  
Crotalus Mitchellii

scholarly journals Syntheses and PDT activity of new mono- and di-conjugated derivatives of chlorin e6

2017 ◽  
Vol 21 (04-06) ◽  
pp. 354-363 ◽  
Author(s):  
Hui Chen ◽  
Stewart W. Humble ◽  
R. G. Waruna Jinadasa ◽  
Zehua Zhou ◽  
Alex L. Nguyen ◽  
...  
Keyword(s):  
Amino Acid ◽  
In Vitro Cytotoxicity ◽  
Chlorin E6 ◽  
New Compounds ◽  
Derivatives Of

Syntheses of three new chlorin e6 conjugates for PDT of tumors are reported. One of the new compounds 17 is conjugated with lysine at the 131-position, but the others are mono-conjugated 14 or diconjugated 15 with the non-amino acid species ethanolamine. Cellular experiments with the three new compounds and previously synthesized non-amino acid 152-conjugates (7–10), 131-monoconjugates 14, 16, and a 131,152-diconjugate 12 are reported. In vitro cytotoxicity experiments show that the 131-conjugates are more toxic than the 152-conjugates, and the most toxic derivative (dark- and photo-toxicity) is the 131-ethylenediamine conjugate 11. The most useful PDT photosentitizers appear to be the ethanolamine derivatives, conjugated at the 152- and the 131,152-positions; these show high phototoxicity but relatively low dark toxicity compared with 11, and also the highest dark/photo cytotoxicity ratios.

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.

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