ChemInform Abstract: Synthesis and Biological Properties of 2-Pyrrolidinoethoxy Derivatives of 3,5-Diarylpyrazoles and 2-Pyrazolines.

Based on carbonyl derivatives of 4-substituted-4-butanolides, the appropriate semi- and thiosemicarbazones have been synthesized. It has been found that some representatives of thiosemicarbazones have pronounced algicidal activity against filamentous green alga Cladophora and blue-green alga (cyanobacterium) Synechocystis and some of the semi- and thiosemicarbazones exhibit moderate antitumor activity. The assessment of the antitumor activity of the compounds was carried out using strains of syngeneic and allogeneic tumor systems as test-objects: lymphocytic leukemia P-388, Lewis lung carcinoma, B16 melanoma and Ehrlich’s ascites tumor. It has also been established that some representatives of thiosemicarbazones exhibit antimutagenic properties. It has been reliably proven that with the formation of a thiazole ring, all properties disappear and a new property in the series of thiazololactones is revealed – antibacterial․

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Synthesis of new cyclopeptide analogues of the miuraenamides

Current Organic Synthesis ◽

10.2174/1570179418666210113161550 ◽

2021 ◽

Vol 18 ◽

Author(s):

Sarah Kappler ◽

Andreas Siebert ◽

Uli Kazmaier

Keyword(s):

Natural Products ◽

Biological Properties ◽

Amide Bond ◽

Side Chain ◽

Aromatic Side Chain ◽

Highly Active ◽

C Terminus ◽

Terminal Amino ◽

High Cytotoxicity ◽

Derivatives Of

Introduction: Miuraenamides belong to marine natural compounds with interesting biological properties. Materials and Methods: They initiate polymerization of monomeric actin and therefore show high cytotoxicity by influencing the cytoskeleton. New derivatives of the miuraenamides have been synthesized containing a N-methylated amide bond instead of the more easily hydrolysable ester in the natural products. Results: Incorporation of an aromatic side chain onto the C-terminal amino acid of the tripeptide fragment also led to highly active new miuraenamides. Conclusion: We could show that the ester bond of the natural product miuraenamide can be replaced by an N-methyl amide. The yields in the cyclization step are high and generally much better that with the corresponding esters. On the other hand, the biological activity of the new amide analogs are lower compared to the natural products, but the activity can significantly be increased by incorporation of a p-nitrophenyl group at the C-terminus of the peptide fragment.

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Biological Properties of Schiff Bases and Azo Derivatives of Phenols

Current Organic Chemistry ◽

10.2174/138527209787193774 ◽

2009 ◽

Vol 13 (2) ◽

pp. 124-148 ◽

Cited By ~ 204

Author(s):

Piotr Przybylski ◽

Adam Huczynski ◽

Krystian Pyta ◽

Bogumil Brzezinski ◽

Franz Bartl

Keyword(s):

Schiff Bases ◽

Biological Properties ◽

Azo Derivatives ◽

Derivatives Of

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Chemoenzymatic Synthesis and Some Biological Properties of O-phosphoryl Derivatives of (E)-resveratrol

Natural Product Communications ◽

10.1177/1934578x0800301023 ◽

2008 ◽

Vol 3 (10) ◽

pp. 1934578X0800301 ◽

Cited By ~ 2

Author(s):

Danilo Aleo ◽

Venera Cardile ◽

Rosa Chillemi ◽

Giuseppe Granata ◽

Sebastiano Sciuto

Keyword(s):

Prostate Cancer ◽

Cancer Cells ◽

Binding Affinity ◽

Spectroscopic Investigation ◽

Biological Properties ◽

Chemoenzymatic Synthesis ◽

Prostate Cancer Cells ◽

Phosphoramidite Chemistry ◽

Protective Groups ◽

Derivatives Of

3- O-, 3,5-di- O- and 4′- O-phosphoryl derivatives of ( E)-resveratrol have been obtained following a chemoenzymatic strategy. Variedly acylated resveratrol derivatives have been obtained first by exploiting regioselective properties of Pseudomonas cepacea or Candida antarctica lipases in organic solvents. Each acyl-resveratrol was then phosphorylated by the phosphoramidite chemistry protocol and in sequence freed of protective groups, affording the desired O-phosphoryl derivative. Following UV-absorption spectroscopic investigation on the interaction of the newly synthesized compounds with DNA, 4′- O-phosphorylresveratrol exhibited the best binding affinity. As a result of cytotoxicity tests, 3- O-phosphorylresveratrol was more active than resveratrol against DU 145 prostate cancer cells.

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Synthesis and Biological Evaluation of New Hydrazone Derivatives of Quinoline and Their Cu(II) and Zn(II) Complexes againstMycobacterium tuberculosis

Bioinorganic Chemistry and Applications ◽

10.1155/2015/153015 ◽

2015 ◽

Vol 2015 ◽

pp. 1-14 ◽

Cited By ~ 18

Author(s):

Mustapha C. Mandewale ◽

Bapu Thorat ◽

Dnyaneshwar Shelke ◽

Ramesh Yamgar

Keyword(s):

Mycobacterium Tuberculosis ◽

Metal Complexes ◽

Inhibitory Activity ◽

Biological Properties ◽

Biological Evaluation ◽

Fluorescence Properties ◽

Synthesis And Biological Evaluation ◽

Derivatives Of

A new series of quinoline hydrazone derivatives and their metal complexes have been synthesized and their biological properties have been evaluated againstMycobacterium tuberculosis(H37 RV strain). Most of the newly synthesized compounds displayed 100% inhibitory activity at a concentration of 6.25–25 μg/mL, againstMycobacterium tuberculosis. Fluorescence properties of all the synthesized compounds have been studied.

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