Synthesis and Antiproliferative Activity of Spirocyclic Cyclodipeptides, Derivatives of 1-Amino-1-cyclobutanecarboxylic Acid

1993 ◽  
Vol 58 (12) ◽  
pp. 2987-2993 ◽  
Author(s):  
Jarmila Vinšová ◽  
Karel Kosař ◽  
Evžen Kasafírek
Keyword(s):  
Amino Acids ◽  
General Formula ◽  
Antiproliferative Activity ◽  
Screening Test ◽  
Proliferative Activity ◽  
Lower Activity ◽  
Chick Embryos ◽  
Cyclobutanecarboxylic Acid ◽  
Derivatives Of

A series of chiral spirocyclic cyclodipeptides of the general formula I was synthesized; the aim was to determine how the substitution of cyclobutane for cyclopentane in cyclo(-alanyl-1-amino-1-cyclopentanecarbonyl-) would influence the inhibition of the proliferative activity of the caudal morphogenic system (CMS) of Chick embryos. Spirocyclic cyclodipeptides Ia - Il were obtained by cyclization of linear dipeptides IIa - IIf, prepared by condensation of protected amino acids by DCCI method. The inhibition was investigated by the Chick Embryotoxicity Screening Test. The results show generally lower activity in the tested series, as compared with derivatives containing 1-amino-1-cyclopentanecarboxylic acid.

Spirocyclic Dipeptides of 1-Amino-1-cyclohexanecarboxylic Acid

1994 ◽  
Vol 59 (1) ◽  
pp. 195-202 ◽  
Author(s):  
Jarmila Vinšová ◽  
Karel Kosař ◽  
Evžen Kasafírek
Keyword(s):  
General Formula ◽  
Screening Test ◽  
Methyl Esters ◽  
Cyclohexanecarboxylic Acid ◽  
Cyclobutanecarboxylic Acid

Spirocyclic cyclodipeptides with 1-amino-1-cyclohexanecarboxylic acid of the general formula cyclo(-Ach-A-), where A is Gly, L-Ala, D-Ala, L-Val, D-Val, L-Leu, D-Leu, D-Pgl, L-Phe or D-Phe, have been prepared by cyclization of the corresponding linear dipeptide methyl esters. The peptides cyclo(-L- or D-Ala-Ach-), cyclo(-L-Val-Ach-) and cyclo(-D-Leu-Ach-) show higher activity in the Chick Embryotoxicity Screening Test when compared with derivatives containing 1-amino-1-cyclopentanecarboxylic acid or 1-amino-1-cyclobutanecarboxylic acid.

Antiproliferative Activity of Derivatives of trans-Bis(salicylaldoximato)copper(II) in vitro. Some in vivo Properties of the Parent Compound

1986 ◽  
Vol 41 (9-10) ◽  
pp. 951-955 ◽  
Author(s):  
Hannu Elo ◽  
Paavo Lumme
Keyword(s):  
Antiproliferative Activity ◽  
Parent Compound ◽  
Antitumor Agent ◽  
Lower Activity ◽  
Pyridoxal Kinase ◽  
Pyridoxal Hydrochloride ◽  
Derivatives Of ◽  
Dihydroxy Derivative

Several derivatives and analogs of the recently reported antiproliferative and antitumor agent trans-bis(salicylaldoximato) copper(II) (CuSAO2) have been prepared and tested for antiproliferative activity against L1210 leukemia cells in vitro. The salicylaldimine analog of CuSAO2 had a very strong antiproliferative activity, the 2-day IC50 value being lower than 3 μg/ml- The 2,3-dihydroxybenzaldoxime analog was equally active with CuSAO2, while the corresponding 2,5-dihydroxy derivative had a slightly lower activity. The 2,3,4-trihydroxybenzaldoxime derivative had a much lower activity than had the dihydroxybenzaldoxime derivatives. The zinc(II) analog of CuSAO2 had only a low antiproliferative activity. The ligand of CuSAO2, salicylaldoxime, resembles pyridoxal oxime, a vitamin B6 antagonist and a powerful inhibitor of pyridoxal kinase. An attempt to reduce the toxicity of CuSAO2 in vivo with pyridoxal hydrochloride led to increased toxicity.

Toxicity of Para-Chloro Substituted Benzene Derivatives in the Microtox™ Test

1985 ◽  
Vol 20 (2) ◽  
pp. 36-43 ◽  
Author(s):  
Klaus L.E. Kaiser ◽  
Juan M. Ribo ◽  
Brian M. Zaruk
Keyword(s):  
General Formula ◽  
Functional Group ◽  
Structural Parameters ◽  
Systematic Investigation ◽  
Photobacterium Phosphoreum ◽  
Benzene Derivatives ◽  
Quantitative Structure ◽  
Chlorinated Benzenes ◽  
Chloro Derivatives ◽  
Derivatives Of

Abstract This paper gives the results of part of a systematic investigation into contaminant toxicity to Photobacterium phosphoreum in the Microtox™ test. Reported are the toxicity values for 39 para-chloro substituted benzene derivatives of the general formula l-Cl-C6h4-4-X=CH2CH(NH2)COOH, F, SO2NH2, OCH2COOH, CH2COOH, CONHNH2, NHCOCH3, CONH2, CH=CHCOOH, SeOOH, CH2NH2, CH2CH2NH2, NO2, H, CF3, CHO, CH2OH, OH, CH3, CCl3, COCH3, COOH, NH2, SO2C6H5, Cl, CH2COCH3, COCl, CN, OCH3, NCO, NHCH3, I, COC6H5, CH2Cl, SH, CH2SH, NCS, CH2CN and SO2C6H4Cl. Except for the last compound, whose solubility is below the required concentration, the toxicities increase in the presented order with a total range of more than three orders of magnitude. The data are discussed in terms of quantitative structure-toxicity correlations with compound-specific structural parameters. In combination with a previously developed submodel on chlorinated benzenes, phenols, nitrobenzenes and anilines, the observed relationships allow the prediction of the toxicity of some 780 possible chloro derivatives of the general formula C6H5-nClnX, where n=<5 and X is a functional group as listed above.

scholarly journals Explicit, Determinantal, and Recurrent Formulas of Generalized Eulerian Polynomials

Axioms ◽  
2021 ◽  
Vol 10 (1) ◽  
pp. 37
Author(s):  
Yan Wang ◽  
Muhammet Cihat Dağli ◽  
Xi-Min Liu ◽  
Feng Qi
Keyword(s):  
General Formula ◽  
Bell Polynomials ◽  
Eulerian Polynomials ◽  
Differentiable Functions ◽  
Faà Di Bruno Formula ◽  
Derivatives Of

In the paper, by virtue of the Faà di Bruno formula, with the aid of some properties of the Bell polynomials of the second kind, and by means of a general formula for derivatives of the ratio between two differentiable functions, the authors establish explicit, determinantal, and recurrent formulas for generalized Eulerian polynomials.

scholarly journals Synthesis, Antiproliferative Activity and Radical Scavenging Ability of 5-O-Acyl Derivatives of Quercetin

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1608
Author(s):  
Stephen Lo ◽  
Euphemia Leung ◽  
Bruno Fedrizzi ◽  
David Barker
Keyword(s):  
Antiproliferative Activity ◽  
Biological Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Breast Cancer Cell Lines ◽  
Scavenging Activity ◽  
Plant Materials ◽  
Wide Range ◽  
Derivatives Of ◽  
Acyl Derivatives

Quercetin is a flavonoid that is found in many plant materials, including commonly eaten fruits and vegetables. The compound is well known for its wide range of biological activities. In this study, 5-O-acyl derivatives of quercetin were synthesised and assessed for their antiproliferative activity against the HCT116 colon cancer and MDA-MB-231 breast cancer cell lines; and their radical scavenging activity against the 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical cation and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical species. Four derivatives were found to have improved the antiproliferative activity compared to quercetin whilst retaining radical scavenging activity.

Derivatives of aminoquinones with N-protected amino acids

1998 ◽  
Vol 5 (4) ◽  
pp. 259-262 ◽  
Author(s):  
Chrysostomos Pachatouridis ◽  
Elias A. Couladouros ◽  
Vassilios P. Papageorgiou ◽  
Maria Liakopoulou-Kyriakides
Keyword(s):  
Amino Acids ◽  
Derivatives Of
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