Methodology for awakening the potential secondary metabolic capacity in actinomycetes

• Shun Saito and
• Midori A. Arai

Beilstein J. Org. Chem. 2024, 20, 753–766, doi:10.3762/bjoc.20.69

• ]. Nocarjamide exhibited biological activity by activating Wnt signaling at an effective concentration of 20–40 μM. Wnt signaling plays an important role in a number of vital processes, such as the formation of various tissues and the differentiation/proliferation of eukaryotic cells [122]. It is interesting

Site-selective reactions mediated by molecular containers

• Rui Wang and
• Yang Yu

Beilstein J. Org. Chem. 2022, 18, 309–324, doi:10.3762/bjoc.18.35

• -selective Diels–Alder and [2 + 2]-photoaddition reactions between 2 and 2,3-substituted naphthalene 7 mediated by cage host A mentioned above (Figure 2) [48]. Given the reduction of the entropic cost resulting from the effective concentration and preorganization of the guest reactants confined to the

Asymmetric organocatalytic Michael addition of cyclopentane-1,2-dione to alkylidene oxindole

• Estelle Silm,
• Ivar Järving and
• Tõnis Kanger

Beilstein J. Org. Chem. 2022, 18, 167–173, doi:10.3762/bjoc.18.18

• oxindole and the squaramide decreasing the effective concentration of the catalyst. Taking this into consideration, 2 equiv of substituted oxindole was used and the reaction proceeded smoothly in 2 h in high enantioselectivity (90%/94% ee), in high yield (74%) but in moderate diastereoselectivity (Table 1

Host–guest interaction and properties of cucurbit[8]uril with chloramphenicol

• Lin Zhang,
• Jun Zheng,
• Guangyan Luo,
• Xiaoyue Li,
• Yunqian Zhang,
• Zhu Tao and
• Qianjun Zhang

Beilstein J. Org. Chem. 2021, 17, 2832–2839, doi:10.3762/bjoc.17.194

• , pH 6.8). Thermodynamic parameters related to the CPE@Q[8] system at 25 °C. Changes in1H NMR chemical shift of CPE after the addition of Q[8] (VD2O/VDCl = 3:2). The minimum effective concentration (MIC) of CPE, CPE@Q[8] against E. coli and S. aureus. Supporting Information Supporting Information File

A comprehensive review of flow chemistry techniques tailored to the flavours and fragrances industries

• Guido Gambacorta,
• James S. Sharley and
• Ian R. Baxendale

Beilstein J. Org. Chem. 2021, 17, 1181–1312, doi:10.3762/bjoc.17.90

Automated high-content imaging for cellular uptake, from the Schmuck cation to the latest cyclic oligochalcogenides

• Rémi Martinent,
• Javier López-Andarias,
• Dimitri Moreau,
• Yangyang Cheng,
• Naomi Sakai and
• Stefan Matile

Beilstein J. Org. Chem. 2020, 16, 2007–2016, doi:10.3762/bjoc.16.167

• constant number of selected cells based on the above criteria, with an increasing concentration, revealed that complex 25 is not toxic up to 20 µM (Figure 9a, black). The effective concentration of 25 obtained with the mitochondria mask was CP50 = 7.3 ± 0.5 μM (Figure 9a and Figure 9b, yellow). With the

Photoreversible stretching of a BAPTA chelator marshalling Ca²⁺-binding in aqueous media

• Aurélien Ducrot,
• Arnaud Tron,
• Robin Bofinger,
• Ingrid Sanz Beguer,
• Jean-Luc Pozzo and
• Nathan D. McClenaghan

Beilstein J. Org. Chem. 2019, 15, 2801–2811, doi:10.3762/bjoc.15.273

• of free calcium is in principle sufficient to induce a contraction (resting concentration of Ca2+ being 0.19–0.28 μM), but that the effective concentration should be much higher as the fibers themselves can buffer free calcium. This was effectively achieved (non-reversibly) with mM concentrations of

Sugar-derived oxazolone pseudotetrapeptide as γ-turn inducer and anion-selective transporter

• Sachin S. Burade,
• Sushil V. Pawar,
• Tanmoy Saha,
• Navanath Kumbhar,
• Amol S. Kotmale,
• Manzoor Ahmad,
• Pinaki Talukdar and
• Dilip D. Dhavale

Beilstein J. Org. Chem. 2019, 15, 2419–2427, doi:10.3762/bjoc.15.234

• within 200 s (Figure 6B), while oxazolone pseudodipeptide 1 was found to be lesser active (Figure 6A). From the dose–response data of 2a, the calculated effective concentration EC50 = 0.72 µM indicated good ion transport activity of 2a (Figure S12 in Supporting Information File 1). The Hill coefficient n

On the design principles of peptide–drug conjugates for targeted drug delivery to the malignant tumor site

• Eirinaios I. Vrettos,
• Gábor Mező and
• Andreas G. Tzakos

Beilstein J. Org. Chem. 2018, 14, 930–954, doi:10.3762/bjoc.14.80

• deactivation through deamination in its inactive metabolite dFdU, the acquired multidrug resistance (MDR) and its high hydrophilicity deterring its prolonged drug release from various vehicles [88], which therefore reduces the effective concentration of gemcitabine. It enters cells through nucleoside

Carbohydrate inhibitors of cholera toxin

• Vajinder Kumar and
• W. Bruce Turnbull

Beilstein J. Org. Chem. 2018, 14, 484–498, doi:10.3762/bjoc.14.34

• ligand group dissociates from the protein, then the others will continue to make contact between the protein and the inhibitor, thus maintaining a high effective concentration of the dissociated ligand group in the vicinity of the binding site and increasing the probability of rebinding occurring. The

Solid-state studies and antioxidant properties of the γ-cyclodextrin·fisetin inclusion compound

• Joana M. Pais,
• Maria João Barroca,
• Maria Paula M. Marques,
• Filipe A. Almeida Paz and
• Susana S. Braga

Beilstein J. Org. Chem. 2017, 13, 2138–2145, doi:10.3762/bjoc.13.212

• discoloration time was verified to be 20 min. The percentage of remaining DPPH· in solution was then calculated for each concentration of fisetin and γ-CD·fisetin. From the linear section of the concentration–activity curve for each compound (Figure 4), the effective concentration required to scavenge 50% of

Comparing blends and blocks: Synthesis of partially fluorinated diblock polythiophene copolymers to investigate the thermal stability of optical and morphological properties

• Pierre Boufflet,
• Sebastian Wood,
• Jessica Wade,
• Zhuping Fei,
• Ji-Seon Kim and
• Martin Heeney

Beilstein J. Org. Chem. 2016, 12, 2150–2163, doi:10.3762/bjoc.12.205

• unreactive towards KCTP when using 1,2-bis(diphenylphosphino)propane as ligand [32][46][48][49]. This results in a reduced effective concentration of 2 relative to 4, since in the case of 4 the regioselectivity of the monomer activation is over 95% [42]. Gel-permeation chromatography (GPC) measurements in

Biocatalysis for the application of CO₂ as a chemical feedstock

• Apostolos Alissandratos and
• Christopher J. Easton

Beilstein J. Org. Chem. 2015, 11, 2370–2387, doi:10.3762/bjoc.11.259

• , the archetypal super-enzyme for which catalytic rates reach the limits of diffusion [30][31]. CO2 consumed by enzymes is therefore efficiently replenished through rapid HCO3− dehydration (Figure 2). Living organisms have developed various mechanisms to increase the effective concentration of CO2

Influence of length and flexibility of spacers on the binding affinity of divalent ligands

• Susanne Liese and
• Roland R. Netz

Beilstein J. Org. Chem. 2015, 11, 804–816, doi:10.3762/bjoc.11.90

• range as the size of a receptor binding pocket. Keywords: binding affinity; divalent ligand; effective concentration; multivalency; Introduction Multivalency is a common design principle in biological systems. The simultaneous binding of several, relatively weakly binding partners is a widely used

• affinity in the latter case is strongly influenced by the conformational linker properties, which can be conveniently discussed in terms of the effective concentration. The effective concentration describes the local concentration of one ligand unit close to one binding pocket, if the other ligand unit is

• assumed to be bound to the other binding pocket. The effective concentration thus corresponds to the probability that the spacer extends to an end-to-end distance that is equal to d, if spacer–receptor interactions are neglected [20]. In the first section different models for the effective concentration

Design, synthesis and photochemical properties of the first examples of iminosugar clusters based on fluorescent cores

• Mathieu L. Lepage,
• Antoine Mirloup,
• Manon Ripoll,
• Fabien Stauffert,
• Anne Bodlenner,
• Raymond Ziessel and
• Philippe Compain

Beilstein J. Org. Chem. 2015, 11, 659–667, doi:10.3762/bjoc.11.74

• concentrations. In another rare genetic disease, the rescue by multimeric correctors of the mutant CFTR protein implied in cystic fibrosis led to the first report of a multivalent effect for amending protein folding defects in cells [26]. As judged by EC50 (half-maximal effective concentration) values, trivalent

Photovoltaic-driven organic electrosynthesis and efforts toward more sustainable oxidation reactions

• Bichlien H. Nguyen,
• Robert J. Perkins,
• Jake A. Smith and
• Kevin D. Moeller

Beilstein J. Org. Chem. 2015, 11, 280–287, doi:10.3762/bjoc.11.32

• (galvanostatic) electrolysis [4]. When a constant current is passed through an electrolysis cell, the potential at the anode increases until it reaches that of the substrate in solution with the lowest oxidation potential. It then remains constant at that potential until the effective concentration of the

Improving ITC studies of cyclodextrin inclusion compounds by global analysis of conventional and non-conventional experiments

• Eléonore Bertaut and
• David Landy

Beilstein J. Org. Chem. 2014, 10, 2630–2641, doi:10.3762/bjoc.10.275

• 2–8 : These relations are effective for both cell and syringe. In addition, the titrand total concentration may be multiplied by a corrective factor (n), equal to 1 by default, in order to obtain the effective concentration by the use of the fitting procedure. According to the low values of the

Recent progress in the discovery of small molecules for the treatment of amyotrophic lateral sclerosis (ALS)

• Allison S. Limpert,
• Margrith E. Mattmann and
• Nicholas D. P. Cosford

Beilstein J. Org. Chem. 2013, 9, 717–732, doi:10.3762/bjoc.9.82

• cellular toxicity following secondary assays [24]. One of these compounds was chosen for further analysis due to its considerably lower 50% effective concentration (EC50). Interestingly, this selected hit compound, 3-(1H-benzo[d]imidazol-2-yl)-6-chloro-4H-chromen-4-one (052C9, 7; Figure 5), was found to

Surfactant catalyzed convenient and greener synthesis of tetrahydrobenzo[a]xanthene-11-ones at ambient temperature

• Pravin V. Shinde,
• Amol H. Kategaonkar,
• Bapurao B. Shingate and
• Murlidhar S. Shingare

Beilstein J. Org. Chem. 2011, 7, 53–58, doi:10.3762/bjoc.7.9

• substrate molecules. It is suggested that most of the organic substrates are concentrated in these spherical droplets, which act as a hydrophobic reaction sites and results in an increase in the effective concentration of the organic reactants, which might increase the reaction rate via a concentration

The allylic chalcogen effect in olefin metathesis

• Yuya A. Lin and
• Benjamin G. Davis

Beilstein J. Org. Chem. 2010, 6, 1219–1228, doi:10.3762/bjoc.6.140

• sulfide could be explained with a sulfur relayed mechanism (Scheme 9a), where sulfur pre-coordination to the ruthenium center increases the effective concentration between the alkylidene and the alkene substrate. For the allyl sulfides this can occur without detrimental chelation, which is thought to be

A bivalent glycopeptide to target two putative carbohydrate binding sites on FimH

• Thisbe K. Lindhorst,
• Kathrin Bruegge,
• Andreas Fuchs and
• Oliver Sperling

Beilstein J. Org. Chem. 2010, 6, 801–809, doi:10.3762/bjoc.6.90

• different site or to a different protein of the fimbrial shaft, thus lowering its effective concentration. Thus, the hypothesis of multiple binding sites on FimH could not be conclusively supported by testing the new bivalent ligand 1, likewise, neither can our findings be taken as counter-evidence. In

Benzyne arylation of oxathiane glycosyl donors

• Martin A. Fascione and
• W. Bruce Turnbull

Beilstein J. Org. Chem. 2010, 6, No. 19, doi:10.3762/bjoc.6.19

• 20 and 26 in glycosylation reactions with other acceptors prior to acetate glycosylation were in vain, presumably due to the high effective concentration of acetate anions in solution. Therefore, alternative oxidising agents for benzyne formation were also investigated in the hope that glycosylation

Continuous flow enantioselective arylation of aldehydes with ArZnEt using triarylboroxins as the ultimate source of aryl groups

• Julien Rolland,
• Xacobe C. Cambeiro,
• Carles Rodríguez-Escrich and
• Miquel A. Pericàs

Beilstein J. Org. Chem. 2009, 5, No. 56, doi:10.3762/bjoc.5.56

• again on the phenylation reaction of p-tolualdehyde. The results of this study are summarized in Table 2. Bearing in mind the strong acceleration usually observed when reactions are run under continuous flow conditions, due to the higher effective concentration of the catalyst, the use of a smaller