Search results

Search for "inhibition" in Full Text gives 548 result(s) in Beilstein Journal of Organic Chemistry. Showing first 200.

Photophysics and photochemistry of NIR absorbers derived from cyanines: key to new technologies based on chemistry 4.0

  • Bernd Strehmel,
  • Christian Schmitz,
  • Ceren Kütahya,
  • Yulian Pang,
  • Anke Drewitz and
  • Heinz Mustroph

Beilstein J. Org. Chem. 2020, 16, 415–444, doi:10.3762/bjoc.16.40

Graphical Abstract
  • cation radical Sens+• forms Sens back in the cycle. The system exhibited photocatalytic behavior with no big changes of absorption for 90 min under aerobic and anaerobic conditions. However, no polymerization occurred under air showing the inhibition of polymerization by oxygen [81]. This described
PDF
Album
Supp Info
Review
Published 18 Mar 2020

Two antibacterial and PPARα/γ-agonistic unsaturated keto fatty acids from a coral-associated actinomycete of the genus Micrococcus

  • Amit Raj Sharma,
  • Enjuro Harunari,
  • Naoya Oku,
  • Nobuyasu Matsuura,
  • Agus Trianto and
  • Yasuhiro Igarashi

Beilstein J. Org. Chem. 2020, 16, 297–304, doi:10.3762/bjoc.16.29

Graphical Abstract
  • well. After incubating for 4 h at 37 °C, the medium was carefully removed by a suction aspirator, and formazan dye, formed by respiratory reduction by living cells, was quantified by the absorption at 450 nm, read by a microplate reader to calculate the rate of cell growth inhibition at each
PDF
Album
Supp Info
Full Research Paper
Published 02 Mar 2020

Synthesis and herbicidal activities of aryloxyacetic acid derivatives as HPPD inhibitors

  • Man-Man Wang,
  • Hao Huang,
  • Lei Shu,
  • Jian-Min Liu,
  • Jian-Qiu Zhang,
  • Yi-Le Yan and
  • Da-Yong Zhang

Beilstein J. Org. Chem. 2020, 16, 233–247, doi:10.3762/bjoc.16.25

Graphical Abstract
  • 2,4-D and the 1,3-dicarbonyl unit, we designed and synthesized a series of novel aryloxyacetic acid derivatives. In this context, these derivatives were subjected to HPPD inhibition, herbicidal activity, crop safety and structure–activity relationship (SAR) studies. As expected, many of the title
  • 13C NMR spectroscopy, and HRMS. Furthermore, the structures of compounds I18 and III4 were verified by X-ray diffractometry (Figure 3). Crystallographic data for crystalline I18 and III4 have been deposited with the Cambridge Crystallographic Data Centre (CCDC 1959130, CCDC 1959152). HPPD inhibition The
  • -withdrawing and electron-donating groups were introduced onto the benzene ring of I1, which significantly influenced the HPPD inhibition activity. We found that electron-withdrawing groups improve the activity; for example, I3 (Ki = 0.36 µM) and I4 (Ki = 0.59 µM) were more potent than I1 (Ki = 1.5 µM) and I2
PDF
Album
Supp Info
Full Research Paper
Published 19 Feb 2020

Potent hemithioindigo-based antimitotics photocontrol the microtubule cytoskeleton in cellulo

  • Alexander Sailer,
  • Franziska Ermer,
  • Yvonne Kraus,
  • Rebekkah Bingham,
  • Ferdinand H. Lutter,
  • Julia Ahlfeld and
  • Oliver Thorn-Seshold

Beilstein J. Org. Chem. 2020, 16, 125–134, doi:10.3762/bjoc.16.14

Graphical Abstract
  • assessment of HITub action We now determined to confirm the mechanism of action of the HITub compounds. To evaluate the biological mechanism of action behind the HITubs’ photoswitchable antimitotic activity, we first checked their inhibition of polymerisation of purified tubulin in a cell-free assay. The
  • results showed almost identical inhibition potency for HITub-4 at c = 10 μM as for the archetypal CDI colchicine at c = 20 μM (Figure S5, Supporting Information File 1), which we took to indicate that (Z)-HITub-4 exerted its bioactivity by specifically binding to tubulin directly in the cell-free system
  • photopharmaceutical tubulin inhibitors, as well as satisfactory photoswitchability of potency. We expect that due to the HITubs’ potency of tubulin inhibition, they will prove a powerful reagent system for biological studies on MT, especially where dark-isomer activity (compared to the currently known, lit-active
PDF
Album
Supp Info
Full Research Paper
Published 27 Jan 2020

Synthesis of C-glycosyl phosphonate derivatives of 4-amino-4-deoxy-α-ʟ-arabinose

  • Lukáš Kerner and
  • Paul Kosma

Beilstein J. Org. Chem. 2020, 16, 9–14, doi:10.3762/bjoc.16.2

Graphical Abstract
  • identified as a major mechanism contributing to antimicrobial resistance of Gram-negative pathogenic bacteria. Inhibition of the corresponding enzymatic steps, specifically the transfer of 4-amino-4-deoxy-ʟ-arabinose, would thus restore the activity of cationic antimicrobial peptides and several
PDF
Album
Supp Info
Full Research Paper
Published 02 Jan 2020

Pigmentosins from Gibellula sp. as antibiofilm agents and a new glycosylated asperfuran from Cordyceps javanica

  • Soleiman E. Helaly,
  • Wilawan Kuephadungphan,
  • Patima Phainuphong,
  • Mahmoud A. A. Ibrahim,
  • Kanoksri Tasanathai,
  • Suchada Mongkolsamrit,
  • Janet Jennifer Luangsa-ard,
  • Souwalak Phongpaichit,
  • Vatcharin Rukachaisirikul and
  • Marc Stadler

Beilstein J. Org. Chem. 2019, 15, 2968–2981, doi:10.3762/bjoc.15.293

Graphical Abstract
  • beauverolide I (5) only exhibited slight inhibition toward the proliferation of the KB3.1 cell line, without either altered or dead cells observed (IC50 20 μg/mL). A number of compounds featuring a dihydrobenzofuran moiety, i.e., the core structure of glycoasperfuran (3), has been reported from endophytic [37
  • effects were further evaluated. Remarkably, the inhibition toward S. aureus and target cell lines was not observed in pigmentosin B (2), but only in pigmentosin A (1). Nevertheless, pigmentosin A (1) displayed anti-S. aureus activity independently from its antibiofilm activity. These properties qualified
  • for their ability to interfere in the biofilm formation of Staphylococcus aureus DSM1104 and Pseudomonas aeruginosa PA14 [51]. The biofilm inhibition assay was performed in 96-well microtiter plates using the microtiter dish biofilm formation assay described by O’Toole [52], with minor modifications
PDF
Album
Supp Info
Full Research Paper
Published 16 Dec 2019

Construction of trisubstituted chromone skeletons carrying electron-withdrawing groups via PhIO-mediated dehydrogenation and its application to the synthesis of frutinone A

  • Qiao Li,
  • Chen Zhuang,
  • Donghua Wang,
  • Wei Zhang,
  • Rongxuan Jia,
  • Fengxia Sun,
  • Yilin Zhang and
  • Yunfei Du

Beilstein J. Org. Chem. 2019, 15, 2958–2965, doi:10.3762/bjoc.15.291

Graphical Abstract
  • of the obtained chromone derivatives was their conversion to chromone-derived natural products. Frutinone A, isolated from the leaves and root bark of Polygala fruticosa, shows various biological activities, including antibacterial, antioxidant, and potent cytochrome P450 1A2 inhibition (CYP1A2, IC50
PDF
Album
Supp Info
Letter
Published 12 Dec 2019

Chemical synthesis of tripeptide thioesters for the biotechnological incorporation into the myxobacterial secondary metabolite argyrin via mutasynthesis

  • David C. B. Siebert,
  • Roman Sommer,
  • Domen Pogorevc,
  • Michael Hoffmann,
  • Silke C. Wenzel,
  • Rolf Müller and
  • Alexander Titz

Beilstein J. Org. Chem. 2019, 15, 2922–2929, doi:10.3762/bjoc.15.286

Graphical Abstract
  • myxobacterium Archangium gephyra (Figure 1) [5][6]. These cyclic peptides have interesting biological activities such as cytotoxic activity presumably via proteasome inhibition and immunomodulatory effects, and they also show good antibiotic effects against P. aeruginosa [7][8][9]. The structure–activity
PDF
Album
Supp Info
Full Research Paper
Published 05 Dec 2019

Bacterial terpene biosynthesis: challenges and opportunities for pathway engineering

  • Eric J. N. Helfrich,
  • Geng-Min Lin,
  • Christopher A. Voigt and
  • Jon Clardy

Beilstein J. Org. Chem. 2019, 15, 2889–2906, doi:10.3762/bjoc.15.283

Graphical Abstract
  • : mutations. Engineering of terpenoid pathways. a) Metabolic network of terpenoid biosynthesis. Toxic intermediates are labeled with skull signs and known enzyme inhibition by intermediates is indicated. Bottleneck enzymes that have been subjected to optimization/engineering are highlighted in bold. Two novel
PDF
Album
Supp Info
Review
Published 29 Nov 2019

Palladium-catalyzed synthesis and nucleotide pyrophosphatase inhibition of benzo[4,5]furo[3,2-b]indoles

  • Hoang Huy Do,
  • Saif Ullah,
  • Alexander Villinger,
  • Joanna Lecka,
  • Jean Sévigny,
  • Peter Ehlers,
  • Jamshed Iqbal and
  • Peter Langer

Beilstein J. Org. Chem. 2019, 15, 2830–2839, doi:10.3762/bjoc.15.276

Graphical Abstract
  • reported diindolofurans 6a–e (Figure 3) [31]. All compounds show significant inhibition of enzyme h-NPP-3 (Table 3) and most of them of the enzyme h-NPP-1. Compound 5a, containing a phenyl substituent, and compound 5e, containing a p-methoxyphenyl group, showed a selective inhibitory response towards
  • contrast, compounds 6d with a methoxy group and 6e with a benzyl group were more active against NPP-3 than against NPP-1. Compounds 5e and 6d with the methoxy functional group showed high inhibition of h-NPP-3. This suggests that the methoxy group could enhance the inhibition of h-NPP-3. Furo[3,2-b,4,5-b
  • ']diindoles 6 exhibited an even stronger activity than derivatives 5 which might be caused by their bigger heterocyclic moiety. All compounds 5 and 6 were active to inhibit enzymes h-NPP-3, which suggests that the furoindole core structure is the main pharmacophore for the inhibition against h-NPP, while
PDF
Album
Supp Info
Full Research Paper
Published 22 Nov 2019

Chemical tuning of photoswitchable azobenzenes: a photopharmacological case study using nicotinic transmission

  • Lorenzo Sansalone,
  • Jun Zhao,
  • Matthew T. Richers and
  • Graham C. R. Ellis-Davies

Beilstein J. Org. Chem. 2019, 15, 2812–2821, doi:10.3762/bjoc.15.274

Graphical Abstract
  • inhibition. It is noteworthy to mention that without puffing any CCh agonist, irradiation of green or violet light did not evoke any detectable currents in patch-clamped cells. Finally, we tested the synthetic precursor of our tetherable t-4FABTA probe (i.e., photochrome 2) as a potential, freely diffusible
PDF
Album
Supp Info
Full Research Paper
Published 21 Nov 2019

An improved, scalable synthesis of Notum inhibitor LP-922056 using 1-chloro-1,2-benziodoxol-3-one as a superior electrophilic chlorinating agent

  • Nicky J. Willis,
  • Elliott D. Bayle,
  • George Papageorgiou,
  • David Steadman,
  • Benjamin N. Atkinson,
  • William Mahy and
  • Paul V. Fish

Beilstein J. Org. Chem. 2019, 15, 2790–2797, doi:10.3762/bjoc.15.271

Graphical Abstract
  • inhibition activity could be achieved, none of these amides demonstrated the required combination of metabolic stability along with cell permeability without evidence of P-gp mediated efflux. Conclusion: Mouse pharmacokinetic studies demonstrate that 1 is unsuitable for use in models of disease where brain
  • 1 (or 17) which combines Notum inhibition with CNS penetration would be a valuable chemical probe for investigating the role of Notum in disease models. Keywords: brain penetration; 1-chloro-1,2-benziodoxol-3-one; electrophilic chlorination; LP-922056; Notum inhibitor; Introduction The Wnt
  • by activation with HBTU and then subsequent reaction with the amine 18 (Scheme 4). These amides 17 were designed to have molecular properties (mw, cLogP, tPSA, HBD, pKa) consistent with CNS drug-like space [20]. Although significant Notum inhibition activity could be achieved (IC50 < 100 nM), none of
PDF
Album
Supp Info
Full Research Paper
Published 19 Nov 2019

Skeletocutins M–Q: biologically active compounds from the fruiting bodies of the basidiomycete Skeletocutis sp. collected in Africa

  • Tian Cheng,
  • Clara Chepkirui,
  • Cony Decock,
  • Josphat C. Matasyoh and
  • Marc Stadler

Beilstein J. Org. Chem. 2019, 15, 2782–2789, doi:10.3762/bjoc.15.270

Graphical Abstract
  • , compound 3 moderately inhibited the biofilm formation of Staphylococcus aureus (S. aureus), while compounds 3 and 4 performed moderately in the ʟ-leucine-7-amido-4-methylcoumarin (ʟ-Leu-AMC) inhibition assay. These compounds represent the first secondary metabolites reported to occur in the fruiting bodies
  • inhibition activity against S. aureus, they showed only weak activity with 20 and 56% inhibition of the biofilm, respectively, at a concentration 256 µg/mL. Tyromycin A (6) was previously reported to be an inhibitor of leucine aminopeptidase in HeLa S3 cells [6]. Accordingly, all compounds 1–5 were tested
  • for their inhibition activity against hydrolysis of ʟ-leucine-7-amido-4-methylcoumarin (ʟ-Leu-AMC). Compound 4 exhibited moderate activity, with an IC50 value of 71.1 µg/mL (Table 3 and Figure 3) when 50 µM of the substrate was used. Compounds 3 and 5 exhibited weak activities, with IC50 values of >80
PDF
Album
Supp Info
Full Research Paper
Published 19 Nov 2019

Plasma membrane imaging with a fluorescent benzothiadiazole derivative

  • Pedro H. P. R. Carvalho,
  • Jose R. Correa,
  • Karen L. R. Paiva,
  • Daniel F. S. Machado,
  • Jackson D. Scholten and
  • Brenno A. D. Neto

Beilstein J. Org. Chem. 2019, 15, 2644–2654, doi:10.3762/bjoc.15.257

Graphical Abstract
  • viability inhibition was determined by evaluation of MTT result obtained for test samples compared with the control samples in the same conditions, following the expression: [survival % = [(tested sample-blank)/(control sample-blank)] × 100]. Bioimaging experiments. The bioimaging experiments were performed
PDF
Album
Supp Info
Letter
Published 06 Nov 2019

Synthesis of novel sulfide-based cyclic peptidomimetic analogues to solonamides

  • José Brango-Vanegas,
  • Luan A. Martinho,
  • Lucinda J. Bessa,
  • Andreanne G. Vasconcelos,
  • Alexandra Plácido,
  • Alex L. Pereira,
  • José R. S. A. Leite and
  • Angelo H. L. Machado

Beilstein J. Org. Chem. 2019, 15, 2544–2551, doi:10.3762/bjoc.15.247

Graphical Abstract
  • since the hemolysin expression is activated by S. aureus QS, we can suppose that the reported activity may be related to the inhibition of this bacterial communication system. Results and Discussion Rational design and synthesis of the solonamide analogues The rational design of our solonamide analogues
  • wavenumber values for the lactone C=O stretch was also observed for bands assigned to the C=C bonds as consequence of their conjugation. Evaluation of the growth inhibition and hemolytic activity of S. aureus for the solonamide analogues Initially, the antibacterial activity of all analogues 9 was tested by
  • , chosen based on the optimal dose observed in the hemolysis inhibition assay. We observed that these two compounds did not affect the fibroblast viability in the concentrations tested (Figure 4). Furthermore, no statistically significant difference was observed between exposition times of 24 and 48 h
PDF
Album
Supp Info
Full Research Paper
Published 25 Oct 2019

α,ß-Didehydrosuberoylanilide hydroxamic acid (DDSAHA) as precursor and possible analogue of the anticancer drug SAHA

  • Shital K. Chattopadhyay,
  • Subhankar Ghosh,
  • Sarita Sarkar and
  • Kakali Bhadra

Beilstein J. Org. Chem. 2019, 15, 2524–2533, doi:10.3762/bjoc.15.245

Graphical Abstract
  • species (ROS) as some apoptotic features. Keywords: anticancer drug; cross metathesis; HDAC inhibition; hydroxamates; reactive oxygen species; Introduction Suberoylanilide hydroxamic acid (SAHA, 1, Figure 1, vorinostat [1][2], has now emerged as a FDA approved drug for the treatment of relapsed and
  • refractory cutaneous T-cell lymphoma (CTCL) [3]. Moreover, it also shows anticancer activity against a large number of hematological and solid malignancies [4][5]. Its anticancer activity is related to inhibition of histone deacetylase inhibitor (HDACi) at nanomolar concentrations (IC50 < 86 nM). Although
  • , originally recognized as a pan-inhibitor, recent studies have established that it is unable to inhibit Class IIA lysine deacetylases (HDAC/4/5/79), thus showing some selectivity profile [6][7]. Moreover, pan-inhibition is also a cause of increased concern due to adverse side effects [8]. The closely related
PDF
Album
Supp Info
Full Research Paper
Published 24 Oct 2019

In search of visible-light photoresponsive peptide nucleic acids (PNAs) for reversible control of DNA hybridization

  • Lei Zhang,
  • Greta Linden and
  • Olalla Vázquez

Beilstein J. Org. Chem. 2019, 15, 2500–2508, doi:10.3762/bjoc.15.243

Graphical Abstract
  • switching capacities and duplex formation were analyzed. Our group has recently demonstrated that photoresponsive peptides can affect the transcription of genes via inhibition of histone-modifying enzymes [37]. Repression of enzymes is achievable at nucleic acid level too. Therefore, in this project we
PDF
Album
Supp Info
Letter
Published 22 Oct 2019

Current understanding and biotechnological application of the bacterial diterpene synthase CotB2

  • Ronja Driller,
  • Daniel Garbe,
  • Norbert Mehlmer,
  • Monika Fuchs,
  • Keren Raz,
  • Dan Thomas Major,
  • Thomas Brück and
  • Bernhard Loll

Beilstein J. Org. Chem. 2019, 15, 2355–2368, doi:10.3762/bjoc.15.228

Graphical Abstract
  • isolated in 1985 from cigarette smoke condensate and identified as anticancer agents [76]. With quite similar potency (α-CBT: 25.2 µM and β-CBT: 21.9 µM [77]), they showed inhibition of the induction of Epstein–Barr virus early antigen by lymphoblastoid cancer cells. In the tobacco plant itself, both
PDF
Album
Review
Published 02 Oct 2019

Isolation and biosynthesis of an unsaturated fatty acid with unusual methylation pattern from a coral-associated bacterium Microbulbifer sp.

  • Amit Raj Sharma,
  • Enjuro Harunari,
  • Tao Zhou,
  • Agus Trianto and
  • Yasuhiro Igarashi

Beilstein J. Org. Chem. 2019, 15, 2327–2332, doi:10.3762/bjoc.15.225

Graphical Abstract
  • . Compound 1 showed weak growth inhibition against Saccharomyces cerevisiae. Keywords: biosynthesis; fatty acid; marine bacteria; methylation; Microbulbifer; Introduction Marine microbial symbionts are currently recognized as a reservoir of new bioactive compounds [1]. The most well-studied host animal is
PDF
Album
Supp Info
Full Research Paper
Published 30 Sep 2019

Synthesis of acremines A, B and F and studies on the bisacremines

  • Nils Winter and
  • Dirk Trauner

Beilstein J. Org. Chem. 2019, 15, 2271–2276, doi:10.3762/bjoc.15.219

Graphical Abstract
  • ) exhibited no significant bioactivity, acremines A–D showed inhibition of P. viticola sporangia germination. In 2015, Wei and co-workers discovered bisacremines E–G, the most complex members of the acremine family, from the soil-derived strain A. persicinum SC0105 [4]. These natural products are presumed to
PDF
Album
Supp Info
Full Research Paper
Published 23 Sep 2019

Isolation of fungi using the diffusion chamber device FIND technology

  • Benjamin Libor,
  • Henrik Harms,
  • Stefan Kehraus,
  • Ekaterina Egereva,
  • Max Crüsemann and
  • Gabriele M. König

Beilstein J. Org. Chem. 2019, 15, 2191–2203, doi:10.3762/bjoc.15.216

Graphical Abstract
  • . alpina and I. europaea inhibited the growth of B. megaterium, i.e., inhibition zones of 1, 2, 1.5, 1, 4, 5, 5 and 3 mm were reached, respectively (streptomycin, equally concentrated, was used as positive control with an inhibition zone of 10 mm). Additionally, the extract of I. europaea inhibited the
  • growth of M. violaceum with an inhibition zone of 3 mm in diameter (miconazole, half concentrated, was used as positive control with an inhibition zone of 10 mm; see Supporting Information File 1, Table S3 for full experimental data). Detailed chemical investigation of H. cf. alpina including structure
  • TSB (Tryptic soy broth, Oxoid) growth suspension of the bacteria to be tested. Compounds were diluted to a concentration of 1 mg/mL (syringomycin 0.5 mg/mL) with DMSO and 3 µL of this dilution were placed on the surface of the agar. Compounds diffuse into the agar and the size of the inhibition zone
PDF
Album
Supp Info
Full Research Paper
Published 19 Sep 2019

Azologization and repurposing of a hetero-stilbene-based kinase inhibitor: towards the design of photoswitchable sirtuin inhibitors

  • Christoph W. Grathwol,
  • Nathalie Wössner,
  • Sören Swyter,
  • Adam C. Smith,
  • Enrico Tapavicza,
  • Robert K. Hofstetter,
  • Anja Bodtke,
  • Manfred Jung and
  • Andreas Link

Beilstein J. Org. Chem. 2019, 15, 2170–2183, doi:10.3762/bjoc.15.214

Graphical Abstract
  • pan-sirtuin inhibitor nicotinamide (Figure 1). Likewise Sirt2 inhibition was shown to have beneficial effects in animal and cell models of neurodegenerative diseases like HD and Parkinson’s disease [11][12]. Sirt3 activity recently was found to play an important role in cardiovascular diseases and
  • azobenzenes are more convenient as already proven by their use as photoswitches in countless biological applications [26][27][28][29][30]. However, their heteroaromatic counterparts still seem underrepresented [31]. The approach to new chemotypes for sirtuin inhibition via known adenosine mimicking kinase
  • in selectivity for Sirt2 and Sirt3 over Sirt1 could be observed for 2c, 4a and 4b. While none of the modifications provided complete isoenzyme specificity, 2c preferentially inhibited Sirt2 (IC50 6.6 ± 0.5) and Sirt3 (IC50 7.5 ± 0.9 µM) compared to Sirt1 (51% inhibition at 100 µM). Though not
PDF
Album
Supp Info
Full Research Paper
Published 16 Sep 2019

Archangelolide: A sesquiterpene lactone with immunobiological potential from Laserpitium archangelica

  • Silvie Rimpelová,
  • Michal Jurášek,
  • Lucie Peterková,
  • Jiří Bejček,
  • Vojtěch Spiwok,
  • Miloš Majdl,
  • Michal Jirásko,
  • Miloš Buděšínský,
  • Juraj Harmatha,
  • Eva Kmoníčková,
  • Pavel Drašar and
  • Tomáš Ruml

Beilstein J. Org. Chem. 2019, 15, 1933–1944, doi:10.3762/bjoc.15.189

Graphical Abstract
  • the range of nanomoles [3]. The inhibition of SERCA by thapsigargin is stoichiometric and irreversible [4] and results in the depletion of the intracellular calcium storage and an elevated cytosolic calcium concentration, which then can trigger apoptosis in cells. This ability of thapsigargin to
  • In order to reveal whether compound 1 is as potent as thapsigargin or compound 2 in terms of inhibition of cancer cell proliferation, we evaluated its cytotoxicity in a number of cell lines originating from various tumors: prostate, osteosarcoma, breast, colon, pancreas and lung. Cells were treated
  • Figure 6. Considering the inhibition potency of SERCA by thapsigargin and compound 2 [7][23] we are not convinced that the missing structural moiety O-2-octanoyl (see Figure 6, A) in the case of compound 1 and 2 has a significant influence on the affinity to SERCA. Furthermore, the O-8 butanoyl and O-10
PDF
Album
Supp Info
Full Research Paper
Published 13 Aug 2019

Design, synthesis and biological evaluation of immunostimulating mannosylated desmuramyl peptides

  • Rosana Ribić,
  • Ranko Stojković,
  • Lidija Milković,
  • Mariastefania Antica,
  • Marko Cigler and
  • Srđanka Tomić

Beilstein J. Org. Chem. 2019, 15, 1805–1814, doi:10.3762/bjoc.15.174

Graphical Abstract
  • for target inhibition of liver metastasis [51]. Therefore, the presented mannosylated desmuramyl peptides with incorporated adamantane will be further explored in order to get a better insight into possible PRR crosstalk. Namely, inclusion of adamantane into carriers such as liposomes can additionally
PDF
Album
Supp Info
Full Research Paper
Published 29 Jul 2019

A golden opportunity: benzofuranone modifications of aurones and their influence on optical properties, toxicity, and potential as dyes

  • Joza Schmitt and
  • Scott T. Handy

Beilstein J. Org. Chem. 2019, 15, 1781–1785, doi:10.3762/bjoc.15.171

Graphical Abstract
  • non-toxic, although data reported in the literature shows considerable variability even in this respect. An initial screening of toxicity was conducted at a fairly high concentration (200 μM) on the present series of compounds using a standard HEP G2 inhibition assay (Table 1). Compared to a currently
  • used yellow dye (tartrazine), the aurones are similar to more toxic. Within the aurone series, though, an interesting pair of trends can be observed. First, all hydroxylated aurones are comparatively more toxic, displaying >50% inhibition at 200 μM. Methyl groups are similarly mostly more toxic. For
PDF
Album
Supp Info
Full Research Paper
Published 25 Jul 2019
Other Beilstein-Institut Open Science Activities