Phenolic compounds from Eucalyptus gomphocephala with potential cytotoxic and antioxidant activities

Two new phenolic compounds, 2,4,6-trihydroxy-5-methyl-acetophenone 2-O-beta-D-glucopyranoside (3), and benzyl alcohol 7-O-(3',4',6'-tri-O-galloyl)-beta-D-glucopyranoside (8), together with eight known phenolic compounds, were isolated from the 70% aqueous acetone extract of Eucalyptus gomphocephala DC. (Myrtaceae). The isolated compounds were elucidated based on their 1H, 13C, DQF-COSY, selective 1D-TOCSY, HSQC, and HMBC NMR spectroscopic and ESI-MS data. The antioxidant effect of the phenolic compounds was tested using 1,1-diphenyl-2-picrylhydrazyl (DPPH), hydroxyl radical and super oxide anion radical scavenging assays. The cytotoxicity of the isolated compounds was evaluated using HeLa cell line.     

Facile Access to Benzothiazole‐Containing Pyrrolo[1,2‐a]quinolines and Pyrrolo[2,1‐a]isoquinolines via Nitrogen Ylides

Quinoline and isoquinoline react with 2‐(bromoacetyl)benzothiazole ( 1 ) in dry benzene to give the corresponding quinolinium and isoquinolinium salts 2 and 10 which undergo base‐mediated [3+2] 1,3‐dipolar cycloaddition with some acetylene and ethylene derivatives to give the corresponding benzothiazole‐containing pyrrolo[1,2‐a]quinoline and pyrrolo[2,1‐a]isoquinoline derivatives.     

Design,Synthesis and Anticancer Evaluation of Substituted Cinnamic Acid Bearing 2-Quinolone Hybrid Derivatives

A new series of hybrid molecules containing cinnamic acid and 2-quinolinone derivatives were designed and synthesized. Their structures were confirmed by ¹H-NMR, ¹³C-NMR and mass analyses. All the synthesized hybrid molecules were assessed for their in vitro antiproliferative activity against more than one cancer cell lines. Compound 3-(3,5-dibromo-7,8-dihydroxy-4-methyl-2-oxoquinolin-1(2H)-ylamino)-3-phenylacrylic acid (5a) with IC₅₀ = 1.89 μM against HCT-116 was proved to the most potent compound in this study, as compared to standard drug staurosporin. DNA flow cytometry assay of compound 5a revealed G2/M phase arrest and pre-G1 apoptosis. Annexin V-FITC showed that the percentage of early and late apoptosis was increased. The results of topoisomerase enzyme inhibition activity showed that the hybrid molecule 5a displays potent inhibitory activity compared with control.     

In vitro antioxidant and antiproliferative activities of six international basil cultivars

The total phenolic, flavonoid and tannin contents in leaves extracts of Ocimum basilicum (OB) (Lamiaceae) international cultivars, as well as their overall antioxidant activities using DPPH and linoleic acid assays, were investigated. Furthermore, the antiproliferative and cytotoxic activities against line HeLa, MCF-7, Jurkat, HT-29, T24, MIAPaCa-2 cancer cells and one normal human cell line HEK-293 were examined. DPPH and linoleic acid assays ranged from 75.8% to 93.3% and from 74.5% to 97.1%; respectively. O. b. ‘purple ruffle’, O. b. ‘dark opale’, O. b. ‘genovese’, O. b. ‘anise’, O. b. ‘bush green’ and O. b. L. (OBL) varied in their antiproliferative and cytotoxic activities, influenced cell cycle progression and stimulated apoptosis in most cancer cells. OBL exhibited the highest antioxidant and antiproliferative activities. OB extracts not only improve taste but also have certain anticancer activity against diverse cancer cells due to the presence of compounds such as rosmarinic acid, chicoric acid and caftaric acid. Thus, OB represents a potent source of anticancer materials.     

Synthesis and anticancer activity of novel 2-substituted pyranopyridine derivatives

Research on Chemical Intermediates - A novel series of 2-aminopyranopyridine derivatives (3–19) were synthesized utilizing...     

Antimicrobial,antioxidant and antitumor activities of Nano-Structure Eu (III) and La (III) complexes with nitrogen donor tridentate ligands

Nano structure metal complexes of Eu (III) and La (III) with two different nitrogen donor tridentate ligands: N-(2-Aminoethyl)-1,3-propanediamine “AEPD = L1” and 1-(2-Aminoethyl)piperazine “AEPz = L2” , were prepared. All synthesized compounds were identified and confirmed by elemental analyses, molar conductivity and spectral analyses (UV–Visible, IR and mass). Conductance measurement indicates that all the complexes are non-electrolytic in nature and the complexes were isolated in 1:1 molar ratio (metal: ligand). Thermal decomposition profiles were consistent with the proposed formulations. The ligands behave as a tridentate ligand through three nitrogen centers of donation. The nano-size was investigated by using transmission electron microscopy (TEM). The geometric structure properties were analyzed using density functional theory (DFT) for ligands and their Lanthanum (III) complexes. The complexes were screened against some bacteria strains, hepatocellular cell line and diphenylhydrazine free radical. The molecular docking active sites interactions were evaluated.     

Facile Novel Synthesis and Reactions of Thiazolidin-4-one Derivatives for Antimicrobial Agents

A facile and fast procedure for synthesis of 3-phenyl-cyclohexane(1′-2)thiazolidin-4-one (1), which underwent condensation with glucose and p-chlorobenzaldehyde to afford 2 and 3, respectively. Compound 3 was used as precursor for the preparation of some fused heterocyclic compounds 4–7. Compound 4 was alkylated using dichloroacetone and chloroacetic acid to afford 8 and 9, respectively. Also, it reacted with acrylonitrile and hydrazine hydrate to afford 10 and 11, respectively. Compound 9 was condensed with p-chlorobenzaldehyde and glucose to afford 12 and 13, respectively. Selected members of the synthesized compounds were screened for antimicrobial activity.