Search results for "Biological activity"

1-methil-3H-pyrazolo[1-2-a]benzo[1-2-3-4]tetrazin-3-ones, design synthesis and biological activity of new antitumoral agents

2005

1-Methylpyrazolo[1,2-a]benzo[1,2,3,4]tetrazin-3-ones 4, synthesized in good to excellent yields, were designed as novel alkylating agents because of their peculiar chemical behavior. All derivatives showed antiproliferative activity against more than 50 types of tumor cell lines with GI50 reaching sub-micromolar values. SAR studies revealed that the presence of a chlorine atom is well-tolerated in both positions 8 and 9, whereas in the case of the methyl group, switching from the 8 to the 9 position gives rise to the most active compound of the series, 4g, either for the number of cell lines inhibited and for selectivity against leukaemia and renal cancer subpanels. COMPARE and 3D-MIND comp…

ChemInform Abstract: Non-Steroidal Antiinflammatory Agents. Part 23. Synthesis and Pharmacological Activity of Enaminones which Inhibit Both Bovine C…

2010

Syntheses of Some Biologically Active Compounds from Stilbenes Isolated from the Bark ofPicea abies

1992

From the four stilbenes 1–4 isolated from the bark of Picea abies seven compounds 5–11 were obtained by hydrogenation or permethylation. 1H-, 13C-NMR and mass spectra were used for their characterization. The antileukemic activity of each compound was preliminary tested. Some compounds were further tested for their anti-HIV activity.

Supercritical Algal Extracts: A Source of Biologically Active Compounds from Nature

2015

The paper discusses the potential applicability of the process of supercritical fluid extraction (SFE) in the production of algal extracts with the consideration of the process conditions and yields. State of the art in the research on solvent-free isolation of biologically active compounds from the biomass of algae was presented. Various aspects related with the properties of useful compounds found in cells of microalgae and macroalgae were discussed, including their potential applications as the natural components of plant protection products (biostimulants and bioregulators), dietary feed and food supplements, and pharmaceuticals. Analytical methods of determination of the natural compou…

Herbicidal activity of derivatives of 9-aminofluoren-9-ylphosphonic acid

1991

A series of derivatives of 9‐aminofluoren‐9‐ylphosphonic acid (phosphonic analogues of morphactins) were synthesized and screened for herbicidal activity against Lepidium sativum, Cucumis sativus and Lycopersicon esculentum. Ethyl 9‐(N‐alkylamino)fluoren‐9‐yl(phenyl)phosphinates appeared to be equipotent with glyphosate and thus may be recognized as new lead compounds for further structural modifications.

Antifeedant activity of neo-clerodane diterpenoids from Teucrium fruticans and derivatives of fruticolone

1999

The antifeedant activity of three neo-clerodane diterpenoids, fruticolone, isofruticolone and fruticolide from Teucrium fruticans was assessed using larvae of Spodoptera littoralis. Isofruticolone was one of the most potent of the Teucrium derived neo-clerodanes. Chemical modification of functional groups on fruticolone showed that its activity could be enhanced.

Use of molecular topology in the selection of new cytostatic drugs

2000

Abstract Connectivity indices are the topological descriptors that are able to predict different chemical and biological properties of the organic compounds. Recently, our research group has demonstrated their usefulness in selecting new cytostatic compounds, all of them showing antibacterial activity. In this paper we realize that this ability is considerably increased by using our home-made pharmacological distribution diagrams (PDDs) together with the topological charge indices, so that the efficient selection of new candidates within heterogeneous sets of compounds is possible. This is a straightforward way for the design and/or selection of new active compounds on virtually any type of…

Organometallic complexes with biological molecues, part 3.in vivo cytotoxicity of diorganotin (IV) chloro and triorganotin (IV) chloro derivatives of…

1994

In order to obtain a continuous source of mitotic metaphases, gill tissue of Aphaius fasciatus (Pisces, Cyprinodontiformes) has been successfully employed. Results gathered after exposure of fish to R2SnClpenG, R3SnClpenGNa, to the parents R2SnCl2, R3SnCl and to penGNa (penGNa = penicillinGNa; R = methyl, butyl and phenyl) suggest that both the parent organotin (IV) chloride and organotin (IV) chloropenG derivatives are toxic while penGNa exerts no significant toxic activity. Essentially, all of the chromosome abnormalities are classifiable as irregularly staining of chromosomes, breakages, side-arm bridges or pseudochiasmata.

ChemInform Abstract: Syntheses of Some Biologically Active Compounds from Stilbenes Isolated from the Bark of Picea abies.

2010

From the four stilbenes 1–4 isolated from the bark of Picea abies seven compounds 5–11 were obtained by hydrogenation or permethylation. 1H-, 13C-NMR and mass spectra were used for their characterization. The antileukemic activity of each compound was preliminary tested. Some compounds were further tested for their anti-HIV activity.

A diterpenoid with antifeedant activity from Scutellaria rubicunda

1999

Abstract Two diterpenoids have been isolated from Scutellaria rubicunda subsp. linneana : (11 S ,13 S ,15 R and S , 16 R ,19 S )-6 α -acetoxy-19-tigloyloxy-2 α ,19;4 α ,18;11,16;15,16-tetraepoxy-neo-clerodan-15-ol (scutecyprol B) and (11 S ,13 S ,15 R and S , 16 R ,19 S )-6 α -acetoxy-2 α ,19;4 α ,18;11,16;15,16-tetra-epoxy-neo-cleroda-15,19,diol (scutalbin C). Both compounds were tested for antifeedant activity against larvae of some species of Lepidoptera. Scutecyprol B shows potent activity at 100 ppm.