Synthesis and properties of 6-alkynyl-5-aryluracils

• Ruben Manuel Figueira de Abreu,
• Till Brockmann,
• Alexander Villinger,
• Peter Ehlers and
• Peter Langer

Beilstein J. Org. Chem. 2024, 20, 898–911, doi:10.3762/bjoc.20.80

• , including pancreatic, breast, and cervical cancers. Zidovudine is effective against retroviruses and is still used today for the prevention and treatment of HIV/AIDS infections. Brivudine is one of the most potent antiviral agents against herpes zoster virus infections (Figure 1) [17][18][19][20]. Given the

Synthesis, optical and electrochemical properties of (D–π)₂-type and (D–π)₂Ph-type fluorescent dyes

• Kosuke Takemura,
• Kazuki Ohira,
• Taiki Higashino,
• Keiichi Imato and
• Yousuke Ooyama

Beilstein J. Org. Chem. 2022, 18, 1047–1054, doi:10.3762/bjoc.18.106

• This work was supported by the Grant-in-Aids for Scientific Research on Innovative Areas “Soft Crystals” (No. 2903) (JSPS KAKENHI Grant No. 18H04520) and the Suga Weathering Technology Foundation.

Synthetic strategies toward 1,3-oxathiolane nucleoside analogues

• Umesh P. Aher,
• Dhananjai Srivastava,
• Girij P. Singh and
• Jayashree B. S

Beilstein J. Org. Chem. 2021, 17, 2680–2715, doi:10.3762/bjoc.17.182

• remarkable reduction in deaths related to HIV/AIDS in the United States due to usage of combination drug therapies [26]. In these combination therapies, ʟ-(−)-2’,3’-dideoxy-3’-thiacytidine (1) is one of the standard components, having an enhanced pharmacological profile over AZT and other dideoxynucleotide

Cryogels: recent applications in 3D-bioprinting, injectable cryogels, drug delivery, and wound healing

• Luke O. Jones,
• Leah Williams,
• Tasmin Boam,
• Martin Kalmet,
• Chidubem Oguike and
• Fiona L. Hatton

Beilstein J. Org. Chem. 2021, 17, 2553–2569, doi:10.3762/bjoc.17.171

• engineering, cell culture and microbiology, or specific chemicals to aid in chemical, environmental, and medicinal filtration, and purification applications [5][19][42][60][61]. This also aids cell immobilisation, putting cryogels forward for potential use in bioreactors [5][42]. Cells can be included within

Natural products in the predatory defence of the filamentous fungal pathogen Aspergillus fumigatus

• Jana M. Boysen,
• Nauman Saeed and
• Falk Hillmann

Beilstein J. Org. Chem. 2021, 17, 1814–1827, doi:10.3762/bjoc.17.124

• treatment and damage to the cell walls while fumagillin aids in immune evasion by reducing ROS levels, degranulation and actin filamentation in neutrophils [60][132]. In nature, several fungal species are known to produce caspofungin which could trigger fumagillin production in natural environments [132

Sustainable manganese catalysis for late-stage C–H functionalization of bioactive structural motifs

• Jongwoo Son

Beilstein J. Org. Chem. 2021, 17, 1733–1751, doi:10.3762/bjoc.17.122

• constitute an important structural modality in small-molecule drugs, such as levonorgestrel (birth control drug), efavirenz (HIV/AIDS treatment), and erlotinib (anticancer). Although step-economical C–H alkynylations have been investigated with 4d and 5d transition metals, 3d metal-catalyzed late-stage C–H

Chemical approaches to discover the full potential of peptide nucleic acids in biomedical applications

• Nikita Brodyagin,
• Martins Katkevics,
• Venubabu Kotikam,
• Christopher A. Ryan and
• Eriks Rozners

Beilstein J. Org. Chem. 2021, 17, 1641–1688, doi:10.3762/bjoc.17.116

Enhanced target cell specificity and uptake of lipid nanoparticles using RNA aptamers and peptides

• Roslyn M. Ray,
• Anders Højgaard Hansen,
• Maria Taskova,
• Bernhard Jandl,
• Jonas Hansen,
• Citra Soemardy,
• Kevin V. Morris and
• Kira Astakhova

Beilstein J. Org. Chem. 2021, 17, 891–907, doi:10.3762/bjoc.17.75

• acquired through the NIH AIDS reagent program and were engineered to express high levels of the HIV-1 coreceptor CCR5 [44]. HEK293T-gp160 cells were a kind gift from Dr. Bing Chen (Harvard, MA), and stably expressed the 92UG037.8 strain of the viral envelope protein, Env [45]. The human brain endothelial

Microwave-assisted multicomponent reactions in heterocyclic chemistry and mechanistic aspects

• Shivani Gulati,
• Stephy Elza John and
• Nagula Shankaraiah

Beilstein J. Org. Chem. 2021, 17, 819–865, doi:10.3762/bjoc.17.71

• between benzimidazole-linked aminopyridine and Lewis acid activated aldehyde which further on nucleophilic addition with substituted isocyanide leads to intermediate B. A 5-exo-dig intramolecular cyclization with isocyanide aids in the formation of the imidazo[1,2-a]pyridine intermediate C. The final

Molecular basis for protein–protein interactions

• Brandon Charles Seychell and
• Tobias Beck

Beilstein J. Org. Chem. 2021, 17, 1–10, doi:10.3762/bjoc.17.1

• that a nucleic acid scaffold aids the assembly by concentrating assembly units and providing additional association energy. Some viral capsids can self-assemble around other scaffolds that mimic the viral genome in charge and size [89] or can also assemble without any scaffold to form empty capsid

Semiautomated glycoproteomics data analysis workflow for maximized glycopeptide identification and reliable quantification

• Steffen Lippold,
• Arnoud H. de Ru,
• Jan Nouta,
• Peter A. van Veelen,
• Magnus Palmblad,
• Manfred Wuhrer and
• Noortje de Haan

Beilstein J. Org. Chem. 2020, 16, 3038–3051, doi:10.3762/bjoc.16.253

• glycoforms as well as modifications of the glycopeptides and aids the optimization of the search space for MS/MS annotation in an iterative manner. Although an MS1-based approach alone allows the identification of more unique glycopeptides as compared to an MS/MS-based approach, a combined workflow is

NMR Spectroscopy of supramolecular chemistry on protein surfaces

• Peter Bayer,
• Anja Matena and
• Christine Beuck

Beilstein J. Org. Chem. 2020, 16, 2505–2522, doi:10.3762/bjoc.16.203

• they have been used to serve as scaffolds for the assembly of protein arrays and crystallization aids [23][24][25][26][27][28]. In addition, a terbiumIII complex termed crystallophore has been developed as a crystallographic nucleation and phasing tool for protein crystallography that can also easily

• larger ordered structures makes especially the larger calixarenes potent “molecular glues” and crystallization aids [23][24][25][26][27][28]. The PAF protein for example did not yield diffracting crystals on its own, but good quality crystals were obtained in the presence of all calix[n]arenes [25]. The

Architecture and synthesis of P,N-heterocyclic phosphine ligands

• Wisdom A. Munzeiwa,
• Bernard Omondi and
• Vincent O. Nyamori

Beilstein J. Org. Chem. 2020, 16, 362–383, doi:10.3762/bjoc.16.35

• N- and/or O-donor atoms [44]. During catalysis the weakly coordinating hard donor atom detaches to give way for the incoming substrate to coordinate to the metal center [45]. This behavior also aids in ligands being able to stabilize low-valent metal states and promote oxidative addition reactions

A chemically contiguous hapten approach for a heroin–fentanyl vaccine

• Yoshihiro Natori,
• Candy S. Hwang,
• Lucy Lin,
• Lauren C. Smith,
• Bin Zhou and
• Kim D. Janda

Beilstein J. Org. Chem. 2019, 15, 1020–1031, doi:10.3762/bjoc.15.100

• States has necessitated the development of new strategies to treat addiction. Monoclonal antibodies and antidrug vaccines provide a tool that both aids addiction management and reduces the potential for overdose. Dual drug vaccines formulated by successive conjugation or by mixture have certain drawbacks

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

• most common anticancer agents used against a wide variety of tumors. It is sold under the brand name Taxol by Bristol-Myers Squibb Company and is FDA approved for the treatment of breast cancer, ovarian cancer, non-small cell lung cancer and AIDS-related Kaposi's sarcoma. The main disadvantages in the

D–A–D-type orange-light emitting thermally activated delayed fluorescence (TADF) materials based on a fluorenone unit: simulation, photoluminescence and electroluminescence studies

• Lin Gan,
• Xianglong Li,
• Xinyi Cai,
• Kunkun Liu,
• Wei Li and
• Shi-Jian Su

Beilstein J. Org. Chem. 2018, 14, 672–681, doi:10.3762/bjoc.14.55

• is a promising acceptor for orange TADF materials, which aids in the design of the TADF behavior and luminescence color of 1 and 2. Owing to the strong electron-withdrawing ability and extended conjugation length of fluorenone unit, the emission peaks of both materials show obvious red-shifts from

Computational methods in drug discovery

• Sumudu P. Leelananda and
• Steffen Lindert

Beilstein J. Org. Chem. 2016, 12, 2694–2718, doi:10.3762/bjoc.12.267

• ) protease is a prime drug target for anti-AIDS therapeutics. In the early 1990s many approved HIV protease inhibitors were developed to target HIV infections using structure-based molecular docking. It was a ground breaking success at that time and made it possible for HIV infected individuals to live

Interactions between cyclodextrins and cellular components: Towards greener medical applications?

• Loïc Leclercq

Beilstein J. Org. Chem. 2016, 12, 2644–2662, doi:10.3762/bjoc.12.261

Ionic liquids as transesterification catalysts: applications for the synthesis of linear and cyclic organic carbonates

• Maurizio Selva,
• Alvise Perosa,
• Sandro Guidi and
• Lisa Cattelan

Beilstein J. Org. Chem. 2016, 12, 1911–1924, doi:10.3762/bjoc.12.181

• 10 minutes), and, most importantly, higher GD selectivity (63% compared to 45% after 30 minutes) under the same reaction conditions. In order to explain such a behavior, a cooperative mechanism for the ionic liquid catalysis was invoked, whereby the electrophilic nitrogen atom aids in activating the

Opportunities and challenges for direct C–H functionalization of piperazines

• Zhishi Ye,
• Kristen E. Gettys and
• Mingji Dai

Beilstein J. Org. Chem. 2016, 12, 702–715, doi:10.3762/bjoc.12.70

• used to treat HIV/AIDS [5]. Gatifloxacin is an important fluoroquinolone antibiotic [6]. Despite the high frequency appearance of piperazines in small-molecule pharmaceuticals, over 80% only contain substituents at the two nitrogen atoms and a very small fraction of them have simple carbon

The aminoindanol core as a key scaffold in bifunctional organocatalysts

• Isaac G. Sonsona,
• Eugenia Marqués-López and
• Raquel P. Herrera

Beilstein J. Org. Chem. 2016, 12, 505–523, doi:10.3762/bjoc.12.50

• also belong to a class of privileged pharmaceutical scaffolds and exhibit different biological activities, as it is the case of Crixivan [37][38], an HIV protease inhibitor which has been employed for AIDS treatment. The thermodynamic unfavorable cis conformation of these compounds represents a

Continuous formation of N-chloro-N,N-dialkylamine solutions in well-mixed meso-scale flow reactors

• A. John Blacker and
• Katherine E. Jolley

Beilstein J. Org. Chem. 2015, 11, 2408–2417, doi:10.3762/bjoc.11.262

• promotes product formation. Within batch or continuous stirred tank reactors an increase in mixing intensity is achieved with optimised impellor design and speed, alongside a reactor designed to disrupt the flow and increase turbulence. Within meso-scale tubular reactors the addition of in-line aids such

Ruthenium indenylidene “1^st generation” olefin metathesis catalysts containing triisopropyl phosphite

• Stefano Guidone,
• Fady Nahra,
• Alexandra M. Z. Slawin and
• Catherine S. J. Cazin

Beilstein J. Org. Chem. 2015, 11, 1520–1527, doi:10.3762/bjoc.11.166

• phosphine/phosphite 1 and phosphine-based Ind-I in the RCM of 4 (lines are visual aids and not curve fits). Synthesis of the mixed phosphine/phosphite complex 1. Synthesis of the bis-phosphite complex 2. Selected bond distances (Å) and angles (°) for 1, 2 and cis-Caz-1. Scope of the reaction employing 1 and

Consequences of the electronic tuning of latent ruthenium-based olefin metathesis catalysts on their reactivity

• Karolina Żukowska,
• Eva Pump,
• Aleksandra E. Pazio,
• Krzysztof Woźniak,
• Luigi Cavallo and
• Christian Slugovc

Beilstein J. Org. Chem. 2015, 11, 1458–1468, doi:10.3762/bjoc.11.158

• and 15. Lines are intended as visual aids. Composition of a reaction mixture after subjecting 16 to 5 mol % cis-5a in xylene, 140 °C. Lines are intended as visual aids. Monomers utilized in model ROMP reactions. Number-average molecular weight (Mn) of poly-21 prepared with initiators 5a, 14 and 15

The synthesis of active pharmaceutical ingredients (APIs) using continuous flow chemistry

• Marcus Baumann and
• Ian R. Baxendale

Beilstein J. Org. Chem. 2015, 11, 1194–1219, doi:10.3762/bjoc.11.134

• its capacity to run as an uninterrupted process is certainly limited by the solid-phase scavengers employed as purification aids. The stoichiometric scavenging capacity of many of these species coupled with their limited loadings does restrict the quantities of material which can be generated in a run