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Search for "bioactivity" in Full Text gives 165 result(s) in Beilstein Journal of Organic Chemistry.
An easily accessible sulfated saccharide mimetic inhibits in vitro human tumor cell adhesion and angiogenesis of vascular endothelial cells
Beilstein J. Org. Chem. 2012, 8, 787–803, doi:10.3762/bjoc.8.89
- oligosaccharide mimetics containing furan as the core molecules to modulate cell–ECM interactions. Especially 3,4-bis{[(β-D-galactopyranosyl)oxy]methyl}furan (BGF) had shown bioactivity by blocking the adhesion of murine B16F10 melanoma cells to murine fibronectin [15]. We have now obtained similar results with
Identification and isolation of insecticidal oxazoles from Pseudomonas spp.
Beilstein J. Org. Chem. 2012, 8, 749–752, doi:10.3762/bjoc.8.85
- A and B. Labeling experiments confirmed their structures and gave initial evidence for a novel biosynthesis pathway of these natural oxazoles. In order to confirm their structure, they were synthesized, which also allowed tests of their bioactivity. Additionally, the bioactivities of the synthesis
- side chains was concluded from a fatty-acid analysis of the producing strain, which showed only straight-chain fatty acids (data not shown). In order to confirm the structure of all oxazole derivatives, to compare their retention times, and to provide enough material for bioactivity tests, oxazoles 3–6
- tested the bioactivity against the human breast-cancer cell line MCF-7, using the XTT assay [18], and against insect hemocytes from the greater wax moth Galleria melonella according to the method described by Proschak et al. [19]. Three oxazole compounds show LD50 [µg ml−1] values against Galleria
Synthesis of szentiamide, a depsipeptide from entomopathogenic Xenorhabdus szentirmaii with activity against Plasmodium falciparum
Beilstein J. Org. Chem. 2012, 8, 528–533, doi:10.3762/bjoc.8.60
- derived from the efficient synthesis enabled additional bioactivity tests leading to the identification of a notable activity against insect cells and Plasmodium falciparum, the causative agent of malaria. Keywords: cyclic depsipeptide; esterification; natural product; szentiamide; Xenorhabdus
- -weight compounds with UV chromophores (e.g., isopropylstilbenes [4], anthraquinones [4], or xenorhabdines [5]. However, bioactivity-based or MS-based screening of crude extracts and culture supernatants led to the identification of larger compounds, such as the PAX peptides [6], the xenortides [7
- bioassays (unpublished data). Nevertheless, no bioactivity has been described for 1 so far. Since we believe that 1 must have a biological function that is simply awaiting its identification, and since the peptide can only be found in small amounts when X. szentirmaii is grown in Luria–Bertani media, we
N-Heterocyclic carbene/Brønsted acid cooperative catalysis as a powerful tool in organic synthesis
Beilstein J. Org. Chem. 2012, 8, 398–402, doi:10.3762/bjoc.8.43
- true as compared to, for example, N-sulfonylimines), N-arylimines are more reactive as compared to N-alkylimines. The question of whether or not N-alkylimines can be deployed successfully in this methodology deserves further elaboration, and may have certain implications with regard to the bioactivity
Computational evidence for intramolecular hydrogen bonding and nonbonding X···O interactions in 2'-haloflavonols
Beilstein J. Org. Chem. 2012, 8, 112–117, doi:10.3762/bjoc.8.12
- interactions; theoretical calculations; Introduction Intermolecular hydrogen bonding (HB) is an interaction governing self-assembly and is responsible for the architecture and organization of molecular aggregates [1], and also ligand–receptor interactions that are responsible for the bioactivity of compounds
Marilones A–C, phthalides from the sponge-derived fungus Stachylidium sp.
Beilstein J. Org. Chem. 2011, 7, 1636–1642, doi:10.3762/bjoc.7.192
- exhibit an equally broad spectrum of bioactivity, including modulation of the central nervous system, protection against brain eschemia, modulation of platelet aggregation and cardiac function, inhibition of smooth muscle cell proliferation, anti-angina activity, and smooth muscle relaxation, as well as
- berghei (see Supporting Information File 1). Interestingly, marilone C (3) showed no activity at 25 µM concentration, indicating that the methyl group 11-CH3 and/or the position of the ketone functionality is essential for this bioactivity. Marilones A, B, and C (1–3) were also tested for cytotoxic
- at the University of North Carolina at Chapel Hill and Project Officer Jamie Driscol at NIMH, Bethesda MD, USA; we kindly thank also the remaining antiviral bioactivity tests performed by the U.S. National Institute of Health drug discovery program, which were supported by contracts NO1-A1-30048
Natural product biosyntheses in cyanobacteria: A treasure trove of unique enzymes
Beilstein J. Org. Chem. 2011, 7, 1622–1635, doi:10.3762/bjoc.7.191
- bioactivity-guided screening techniques towards cytotoxic, multidrug-resistance reversal, antiprotease, antifungal and antiviral activities [5]. Many bioactive metabolites possess a peptide or a macrolide structure, or a combination of both types [6][7][8]. Other metabolites belong to the alkaloid class of
- , including many that are not or only rarely seen in other microorganisms. The potential of cyanobacteria for natural product research thus goes far beyond the exploitation of the bioactivity of the products. Knowledge about the biochemistry of unique enzymes is particularly valuable for synthetic biology
Synthesis of (−)-julocrotine and a diversity oriented Ugi-approach to analogues and probes
Beilstein J. Org. Chem. 2011, 7, 1504–1507, doi:10.3762/bjoc.7.175
- be considered a privileged structural element for bioactivity. Results and Discussion The synthetic approach, illustrated in Scheme 1, starts from Cbz-glutamine 2, which reacted in the presence of dicyclohexylcarbodiimide (DCC) and N-hydroxysuccinimide (NHS) in DMF to afford Cbz-glutarimide 3 in 76
α,β-Aziridinylphosphonates by lithium amide-induced phosphonyl migration from nitrogen to carbon in terminal aziridines
Beilstein J. Org. Chem. 2010, 6, 978–983, doi:10.3762/bjoc.6.110
- acids; aziridines; lithiation; migration; synthetic methods; Introduction The synthesis of aminophosphonic acids and their derivatives has attracted considerable attention, since the presence of such functionality, typically as amino acid surrogates, leads to interesting bioactivity in, for example
Synthesis of gem-difluoromethylenated analogues of boronolide
Beilstein J. Org. Chem. 2010, 6, No. 37, doi:10.3762/bjoc.6.37
- demonstrated that the α,β-unsaturated-δ-lactone moiety plays a key role in the bioactivity of many natural products. This is due to the fact that this unit is an excellent potential Michael acceptor for nucleophilic amino acid residues of the natural receptors interacting with these compounds [16][17][18
Functional properties of metallomesogens modulated by molecular and supramolecular exotic arrangements
Beilstein J. Org. Chem. 2009, 5, No. 54, doi:10.3762/bjoc.5.54
- going to the tetrahedral [Zn(II)] and pentacoordinate Ga(III) to obtain novel, non conventional structures. Moreover, by changing the nature of coordinating ligands and the kinds of substituents, further properties such as luminescence and bioactivity can be promoted at the same time, leading to smart
Mitomycins syntheses: a recent update
Beilstein J. Org. Chem. 2009, 5, No. 33, doi:10.3762/bjoc.5.33
- : antitumour; bioactivity; mitomycin; mitosene; synthesis; Review Introduction The mitomycins pose unique challenges to the synthetic chemist. As S. Danishefsky noted, “The complexity of the problem arises from the need to accommodate highly interactive functionality in a rather compact matrix and to
An expedient synthesis of 5-n-alkylresorcinols and novel 5-n-alkylresorcinol haptens
Beilstein J. Org. Chem. 2009, 5, No. 22, doi:10.3762/bjoc.5.22
- ][17][18][19][20][21]. However, AR are not generally nor readily available. Thus an efficient preparation method is needed for various analytical, metabolic or bioactivity investigations. The critical step in the synthesis of long alkyl chain (≥C15) AR is the formation of C–C bond between the aromatic
Sordarin, an antifungal agent with a unique mode of action
Beilstein J. Org. Chem. 2008, 4, No. 31, doi:10.3762/bjoc.4.31
- fungi by stabilizing the ribosome/EF2 complex. This mode of action is in contrast to typical antifungals, which target the cell membrane. This unusual bioactivity makes sordarin a promising candidate for the development of new fungicidal agents, and provided the motivation for extensive research. Three
- total syntheses (by the Kato, Mander and Narasaka groups), modifications of the glycosyl unit, and changes to the diterpene core (Cuevas and Ciufolini models) will also be discussed in this review. Keywords: antifungal; bioactivity; sordaricin; sordarin; total synthesis; Introduction For
Themed series in organo- fluorine chemistry
Beilstein J. Org. Chem. 2008, 4, No. 11, doi:10.3762/bjoc.4.11
- practiced particularly when tuning the properties of molecules for specialist functions. Of particular prominence is the role fluorine substitution finds in pharmaceutical development [1], and selective fluorination has made a major contribution to the bioactivity of a wide range of agrochemical products [2
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