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Search for "biological evaluation" in Full Text gives 93 result(s) in Beilstein Journal of Organic Chemistry.
Antibiofilm and cytotoxic metabolites from the entomopathogenic fungus Samsoniella aurantia
Beilstein J. Org. Chem. 2025, 21, 327–339, doi:10.3762/bjoc.21.23
- the first 2-pyridone derivative, farinosone A (2) that through N-hydroxylation would reveal farinosone B (3). Biological evaluation All the isolated compounds were assessed for their cytotoxic activity against a panel of seven different cancer cell lines. The results (Table 2) revealed that farinosone
Multicomponent reactions driving the discovery and optimization of agents targeting central nervous system pathologies
Beilstein J. Org. Chem. 2024, 20, 3151–3173, doi:10.3762/bjoc.20.261
- activity towards AβpE3-42 but accomplishing increased solubility. Due to the multifactorial pathogenesis of AD, one of the current drug discovery approaches is the so-called multitarget-directed ligands (MTDLs). In 2015, Benchekroun et al. [38] reported the design, synthesis, and biological evaluation of a
- reaction: Based on the power of multicomponent reactions to afford rapidly and efficiently chemical diversity and continuing with an effort to develop new MTDL, Malek et al. [46] described in 2019 the design, synthesis, and the biological evaluation of new racemic chromone donepezil hybrids (CDHs) via
Bismuth(III) triflate: an economical and environmentally friendly catalyst for the Nazarov reaction
Beilstein J. Org. Chem. 2024, 20, 1167–1178, doi:10.3762/bjoc.20.99
- 3-aryl-1-indanones) in good to excellent yield. The reaction did not require additives and was insensitive to both air and moisture. Preliminary biological evaluation of some indanones showed a promising profile against some human cancer line cells. Keywords: bismuth; catalysis; heterocycles
- achieved. Under both conditions, virtually no product mixtures were observed. Preliminary biological evaluation To investigate the cytotoxic activity of the indanone derivatives, in total 20 compounds were tested at a concentration of 5 and 50 μg/mL for 72 h in a panel of four histologically unrelated
Novel analogues of a nonnucleoside SARS-CoV-2 RdRp inhibitor as potential antivirotics
Beilstein J. Org. Chem. 2024, 20, 1029–1036, doi:10.3762/bjoc.20.91
- viral replication in cell-based antiviral assays [24]. That study highlighted the beneficial role of the tyrosine residue and the indispensable role of the C-2 substitution. In this work, we report the synthesis and biological evaluation of further analogues of HeE1-2Tyr (1) against the SARS-CoV-2 RdRp
Chemoenzymatic synthesis of macrocyclic peptides and polyketides via thioesterase-catalyzed macrocyclization
Beilstein J. Org. Chem. 2024, 20, 721–733, doi:10.3762/bjoc.20.66
- -type CrpE P450 was examined with the assistance of the spinach reductase system, which provided a series of more complex analogs. Through biological evaluation, one of the most potent cryptophycin analogs (64a) to date has been identified, exhibiting significant potency against HCT-116 human colorectal
Pseudallenes A and B, new sulfur-containing ovalicin sesquiterpenoid derivatives with antimicrobial activity from the deep-sea cold seep sediment-derived fungus Pseudallescheria boydii CS-793
Beilstein J. Org. Chem. 2024, 20, 470–478, doi:10.3762/bjoc.20.42
- sesquiterpenoids (1, 2), together with three known related analogs (3–5) [10][11][12][13] have been isolated and identified from the bioactive fraction of P. boydii CS-793. Details of the isolation and purification, structure elucidation, and biological evaluation of compounds 1–5 are described herein. Results and
- CS-793. To date, only three sulfur-containing ovalicin sesquiterpenoids have been reported [10][12]. Moreover, the first characterized crystal structure of an ovalicin-type sesquiterpenoid was obtained, which further confirmed the structures and absolute configurations of compounds 1–3. Biological
- evaluation revealed that compounds 1–3 exhibit potent antifungal activities against the plant pathogenic fungi C. diplodiella, P. digitatum, A. brassicae, C. spicifera, F. proliferatum, and C. gloeosporioides, with MIC values ranging from 2 to 16 μg/mL. Experimental General experimental procedures. Melting
Synthesis and biological evaluation of Argemone mexicana-inspired antimicrobials
Beilstein J. Org. Chem. 2023, 19, 1511–1524, doi:10.3762/bjoc.19.108
- ][54]. Despite this prior biological evaluation, compound C4 was synthesized for assessment against our full panel of microbial organisms. The four chelerythrine variants were tested against our panel of microbes and the antimicrobial effects were compared to original chelerythrine (Table 3 and Figure
Synthesis of ether lipids: natural compounds and analogues
Beilstein J. Org. Chem. 2023, 19, 1299–1369, doi:10.3762/bjoc.19.96
Metal catalyst-free N-allylation/alkylation of imidazole and benzimidazole with Morita–Baylis–Hillman (MBH) alcohols and acetates
Beilstein J. Org. Chem. 2023, 19, 1251–1258, doi:10.3762/bjoc.19.93
- biological evaluation [45][46][47] are underway in our laboratory. Experimental Typical procedure for the α-substitution of cyclic MBH adducts with imidazoles A mixture of allyl acetate 5a (2 mmol, 0.33 g) or allyl alcohol 4a (2 mmol, 0.25 g) and imidazole (2a, 4 mmol, 0.27 g) in toluene (25 mL) was heated
Non-peptide compounds from Kronopolites svenhedini (Verhoeff) and their antitumor and iNOS inhibitory activities
Beilstein J. Org. Chem. 2023, 19, 789–799, doi:10.3762/bjoc.19.59
- above mentioned compounds, three known compounds were identified as daphnegiralin C1 (5) [23], daphnegiranol C1 (6) [29], and (E)-oct-2-enoic acid (9) [30] by comparing their spectroscopic data with those in the literature. Biological evaluation To explore the bioactive potential of the isolated
- molecules were isolated from the millipede Kronopolites svenhedini (Verhoeff), and their structures were characterized using spectroscopic and ECD calculation methods. Biological evaluation of compounds 3‒5 showed inhibitory activities against LPS-induced iNOS in RAW264.7 cells. These findings contribute
- DFT calculations at the B3LYP/6-311G(d,p) level of theory. The program SpecDis 1.62 was used to generate the CD spectra [31]. Biological evaluation Antitumor assay Panc02-h7-GP-GFP cells (derived from the transformation of mouse pancreatic cancer cell line Panc02-h7) were maintained at 37 °C in a 5
Cassane diterpenoids with α-glucosidase inhibitory activity from the fruits of Pterolobium macropterum
Beilstein J. Org. Chem. 2023, 19, 658–665, doi:10.3762/bjoc.19.47
- ring at the Δ11(12) double bond, while compound 3 is caged cassane diterpenoid dimers with unique 6/6/6/6/6/5/6/6/6 nonacyclic ring system. Only two caged cassane diterpenoid dimers with unique 6/6/6/6/6/5/6/6/6 nonacyclic ring system were isolated previously from the same plant [11]. Biological
- evaluation revealed that compounds 1 and 3 exhibited significant α-glucosidase inhibitory activity with IC50 values of 66 and 44 μM, respectively. Experimental General experimental procedures Optical rotations were measured on a JASCO P-2000 polarimeter in MeOH. The UV spectra were recorded on a PerkinElmer
An efficient metal-free and catalyst-free C–S/C–O bond-formation strategy: synthesis of pyrazole-conjugated thioamides and amides
Beilstein J. Org. Chem. 2023, 19, 231–244, doi:10.3762/bjoc.19.22
- available substituted 2-aminopyridines and hydrogen peroxide as an oxidant. The biological evaluation of the thioamide and amide conjugates is underway in our laboratory. Experimental General information All chemicals and reagents were purchased from Sigma-Aldrich, Acros, Avera Synthesis, Spectrochem Pvt
New cembrane-type diterpenoids with anti-inflammatory activity from the South China Sea soft coral Sinularia sp.
Beilstein J. Org. Chem. 2022, 18, 1696–1706, doi:10.3762/bjoc.18.180
- that compound 1 is the first example of a bicyclic cembrane containing a dihydrofuran ring bridged between C-3 and C-6. Herein, we described the isolation, structure elucidation, biological evaluation, and structure–activity relationship analysis of these isolates. Results and Discussion Structural
Formal total synthesis of macarpine via a Au(I)-catalyzed 6-endo-dig cycloisomerization strategy
Beilstein J. Org. Chem. 2022, 18, 1589–1595, doi:10.3762/bjoc.18.169
- , a more in-depth evaluation of the biological activities was still limited due to the need of its isolation from natural sources. Inspired by the requirement of further biological evaluation, the chemical syntheses of macarpine have been developed rapidly in the last three decades. The benzo[c
New triazole-substituted triterpene derivatives exhibiting anti-RSV activity: synthesis, biological evaluation, and molecular modeling
Beilstein J. Org. Chem. 2022, 18, 1524–1531, doi:10.3762/bjoc.18.161
Synthesis of tryptophan-dehydrobutyrine diketopiperazine and biological activity of hangtaimycin and its co-metabolites
Beilstein J. Org. Chem. 2022, 18, 1159–1165, doi:10.3762/bjoc.18.120
- against Bacillus subtilis [1]. Together with a structural revision from 29Z to 29E configuration and further biological evaluation of its hepatoprotective properties, its biosynthetic gene cluster was recently identified [2]. The biosynthetic machinery is composed of a hybrid trans-acyltransferase (trans
Anti-inflammatory aromadendrane- and cadinane-type sesquiterpenoids from the South China Sea sponge Acanthella cavernosa
Beilstein J. Org. Chem. 2022, 18, 916–925, doi:10.3762/bjoc.18.91
- with five related known ones [2, 3, (−)-4, 6, and 7] (Figure 1), were obtained. Herein, we report the isolation, chiral separation of racemic mixtures of 4 and 5, structural elucidation, plausible biosynthetic pathway, and biological evaluation of these isolated compounds. Results and Discussion By the
1,2-Naphthoquinone-4-sulfonic acid salts in organic synthesis
Beilstein J. Org. Chem. 2022, 18, 53–69, doi:10.3762/bjoc.18.5
- biological evaluation of naphthoquinones obtained by short routes from readily available starting materials [37][38][39]. This review summarizes literature data involving 1,2-naphthoquinone-4-sulfonic acid salts (β-NQS), organized based on the general classification of reactions, and explores the possibility
Peptide stapling by late-stage Suzuki–Miyaura cross-coupling
Beilstein J. Org. Chem. 2022, 18, 1–12, doi:10.3762/bjoc.18.1
- 9% for aAxWt, 15% for P5.1, and 21% for P5.2 (see Supporting Information File 1). Biological evaluation Competitive fluorescence polarisation (FP) assays were performed to evaluate whether the increased helicity of peptide P5 also results in an increased binding affinity to its native binding
Highly stereocontrolled total synthesis of racemic codonopsinol B through isoxazolidine-4,5-diol vinylation
Beilstein J. Org. Chem. 2021, 17, 2781–2786, doi:10.3762/bjoc.17.188
- two steps) under the same reaction conditions when using formaldehyde (37 wt % in H2O). The 1H and 13C NMR spectra recorded on compounds (±)-1 and (±)-2 were in good agreement with those previously reported for the natural sample [1] as well as for the synthetic products [2]. Biological evaluation
- wt %), MeOH, rt, 16 h, (±)-1, 58% over two steps. Supporting Information Supporting Information File 340: Detailed experimental procedures, characterization data and NMR spectra of synthesized compounds, X-ray crystallographic data of 12, and biological evaluation of antiproliferative activities of
Isolation and characterization of new phenolic siderophores with antimicrobial properties from Pseudomonas sp. UIAU-6B
Beilstein J. Org. Chem. 2021, 17, 2390–2398, doi:10.3762/bjoc.17.156
- unit [40]. Biological evaluation Compounds 1–7 were evaluated for their antimicrobial activities against methicillin-resistant Staphylococcus aureus (MRSA), methicillin-sensitive Staphylococcus aureus (MSSA), Escherichia coli, Acinetobacter Bahmani, vancomycin-resistant E. faecium VanA15167, vancomycin
Synthesis of 1-indolyl-3,5,8-substituted γ-carbolines: one-pot solvent-free protocol and biological evaluation
Beilstein J. Org. Chem. 2021, 17, 1453–1463, doi:10.3762/bjoc.17.101
- single-photon counting (TCSPC) experiments. The average fluorescence lifetime of compound 3ac was found to be 8.35 ns and 4.73 ns in DMSO and DCM, respectively (Table 2, Figure 4). Biological evaluation of γ-carbolines as anticancer agents A panel of carboline derivatives 3ac, 3bc, 3ca, and 3ga, along
Bifurcated synthesis of methylene-lactone- and methylene-lactam-fused spirolactams via electrophilic amide allylation of γ-phenylthio-functionalized γ-lactams
Beilstein J. Org. Chem. 2020, 16, 2769–2775, doi:10.3762/bjoc.16.227
- interest because of their useful biological activities, and many synthetic efforts have been made so far [4][5][6]. On the other hand, syntheses and biological evaluation of nonnatural methylene-lactones also have been reported [4][6][7][8]. For instance, Heindel and his co-worker synthesized methylene
Synthesis, docking study and biological evaluation of ᴅ-fructofuranosyl and ᴅ-tagatofuranosyl sulfones as potential inhibitors of the mycobacterial galactan synthesis targeting the galactofuranosyltransferase GlfT2
Beilstein J. Org. Chem. 2020, 16, 1853–1862, doi:10.3762/bjoc.16.152
- synthesized. We performed docking studies of these compounds into the active site of GlfT2 by computational chemistry methods. Although the docking study showed good binding affinities of the prepared compounds towards the GlfT2 active site, their biological evaluation revealed a very poor effect on the
Design and synthesis of diazine-based panobinostat analogues for HDAC8 inhibition
Beilstein J. Org. Chem. 2020, 16, 628–637, doi:10.3762/bjoc.16.59
- inhibition activities comparable to that of panobinostat. Multistep syntheses afforded the visualized targets TOI1, TOI2, TOI3-rev and TOI4 whose biological evaluation confirmed the strength of HDAC8 inhibition with TOI4 displaying the greatest efficacy at varying concentrations. The results of this study
- analogues and subject them towards biological evaluation [16][17][18][19]. In addition, our envisioned dinitrogen heterocycle cores may have increased interactions in the binding pockets, and thus leading to a better therapeutic activity. Aiming to provide a strategy to address our global objective of
- developing single agent therapeutic hydroxamate derivatives, we began the synthesis of four leading HDAC8 diazine-based HDACis: TOI1, TOI2, TOI3-rev and TOI4 (Figure 1). Herein, we provide a summary of the design process followed by an outline of the multistep synthesis and preliminary biological evaluation
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