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View article: Adaptation of the Mitsunobu Reaction for Facile Synthesis of Dorsomorphin-Based Library
Adaptation of the Mitsunobu Reaction for Facile Synthesis of Dorsomorphin-Based Library Open
Pyrazolo[1,5-a]pyrimidine is a nitrogen-containing fused heterocycle that imitates the nitrogenous base adenine with varying degrees of reliability. This fact determines its frequent use in drug design, including the development of ATP-com…
View article: Optimization of the Scheme for Decontaminating Continuous Human Cell Cultures with Antibiotics of Different Mechanisms
Optimization of the Scheme for Decontaminating Continuous Human Cell Cultures with Antibiotics of Different Mechanisms Open
The absence of contamination is an important condition for the reliability of the results obtained when conducting experiments on cell cultures. At the same time, long-term cultivation significantly increases the risk of contamination of t…
View article: Cellular Systems for Colorectal Stem Cancer Cell Research
Cellular Systems for Colorectal Stem Cancer Cell Research Open
Oncological diseases consistently occupy leading positions among the most life-threatening diseases, including in highly developed countries. At the same time, the second most common cause of cancer death is colorectal cancer. The current …
View article: Rational Design Problematics of Peptide Nucleic Acids as SARS-CoV-2 Inhibitors
Rational Design Problematics of Peptide Nucleic Acids as SARS-CoV-2 Inhibitors Open
The use of viral protein inhibitors has shown to be insufficiently effective in the case of highly variable SARS-CoV-2. In this work, we examined the possibility of designing agents that bind to a highly conserved region of coronavirus (+)…
View article: Ubiquitin recruiting chimera: more than just a PROTAC
Ubiquitin recruiting chimera: more than just a PROTAC Open
View article: A Visual Compendium of Principal Modifications within the Nucleic Acid Sugar Phosphate Backbone
A Visual Compendium of Principal Modifications within the Nucleic Acid Sugar Phosphate Backbone Open
Nucleic acid chemistry is a huge research area that has received new impetus due to the recent explosive success of oligonucleotide therapy. In order for an oligonucleotide to become clinically effective, its monomeric parts are subjected …
View article: New Insights into Chemoresistance Mediated by Mdm2 Inhibitors: The Benefits of Targeted Therapy over Common Cytostatics
New Insights into Chemoresistance Mediated by Mdm2 Inhibitors: The Benefits of Targeted Therapy over Common Cytostatics Open
The inhibition of the Mdm2-p53 protein–protein interaction is a promising strategy for anticancer therapy. However, the problem of developing secondary chemoresistance in tumors treated with such drugs has not yet been sufficiently studied…
View article: PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AND THEIR BIOLOGICAL ACTIVITY
PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AND THEIR BIOLOGICAL ACTIVITY Open
The pyrazolo[1,5-a]pyrimidine scaffold is a promising target in the field of heterocyclic chemistry due to its unique structure and wide potential for application in medical chemistry. The ability to chemically modify both the pyrazole and…
View article: NMR-Verified Dearomatization of 5,7-Substituted Pyrazolo[1,5-a]pyrimidines
NMR-Verified Dearomatization of 5,7-Substituted Pyrazolo[1,5-a]pyrimidines Open
Tetrahydropyrazolo[1,5-a]pyrimidine (THPP) is an attractive scaffold for designing biologically active compounds. The most obvious way to obtain such compounds is to reduce pyrazolopyrimidines with complex hydrides, because the pyrimidine …
View article: CCDC 2171213: Experimental Crystal Structure Determination
CCDC 2171213: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2171214: Experimental Crystal Structure Determination
CCDC 2171214: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2171215: Experimental Crystal Structure Determination
CCDC 2171215: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2171216: Experimental Crystal Structure Determination
CCDC 2171216: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Is It Possible to Obtain a Product of the Desired Configuration from a Single Knoevenagel Condensation? Isomerization vs. Stereodefined Synthesis
Is It Possible to Obtain a Product of the Desired Configuration from a Single Knoevenagel Condensation? Isomerization vs. Stereodefined Synthesis Open
The biological activity of compounds directly depends on the three-dimensional arrangement of affinity fragments since a high degree of pharmacophore compliance with the binding site is required. 3-Benzylidene oxindoles are privileged stru…
View article: Development of a Reproducible and Scalable Method for the Synthesis of Biologically Active Pyrazolo[1,5-a]pyrimidine Derivatives
Development of a Reproducible and Scalable Method for the Synthesis of Biologically Active Pyrazolo[1,5-a]pyrimidine Derivatives Open
A reproducible and scalable method has been developed for the synthesis of a series of 3,6-substituted pyrazolo[1,5- a ]pyrimidines, which are the basis for the rational design of selective inhibitors of AMP-activated protein kinase. Regar…
View article: ATP Mimetic Attack on the Nucleotide-Binding Domain to Overcome ABC Transporter Mediated Chemoresistance
ATP Mimetic Attack on the Nucleotide-Binding Domain to Overcome ABC Transporter Mediated Chemoresistance Open
Since the problem of transporter-mediated multidrug resistance of tumor cells is becoming increasingly important in cancer therapy, it is necessary to modulate the activity of efflux transporters of the ABC family, among which P-glycoprote…
View article: Analysis of P-Glycoprotein Transport Cycle Reveals a New Way to Identify Efflux Inhibitors
Analysis of P-Glycoprotein Transport Cycle Reveals a New Way to Identify Efflux Inhibitors Open
P-glycoprotein (P-gp) is found to be of considerable interest for the design of drugs capable of treating chemoresistant tumors. This transporter is an interesting target for which an efficient approach has not yet been developed in terms …
View article: metaRE R Package for Meta-analysis of Transcriptome Data to Identify the Cis-regulatory Code behind the Transcriptional Reprogramming
metaRE R Package for Meta-analysis of Transcriptome Data to Identify the Cis-regulatory Code behind the Transcriptional Reprogramming Open
At the molecular level, response to an external factor or an internal condition causes reprogramming of temporal and spatial transcription. When an organism undergoes physiological and/or morphological changes, several signaling pathways a…
View article: Advanced palladium free approach to the synthesis of substituted alkene oxindoles <i>via</i> aluminum-promoted Knoevenagel reaction
Advanced palladium free approach to the synthesis of substituted alkene oxindoles <i>via</i> aluminum-promoted Knoevenagel reaction Open
A synthetic route for the synthesis of C24, as well as for the design of focused libraries of direct AMPK activators was developed based on a convergent strategy.
View article: CCDC 1585543: Experimental Crystal Structure Determination
CCDC 1585543: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …