Results 31 to 40 of about 47,589 (249)

Standardized Chromatographic and Computational Approaches for Lipophilicity Analysis of Five Gliflozin Antidiabetic Drugs in Relation to Their Biological Activity

Molecules
This study represents the first-time experimental analysis of lipophilicity for antidiabetic drugs from the gliflozin class using chromatographic methods alongside computational approaches.
Anna Gumieniczek, Anna Berecka-Rycerz, Marcelina Dul, Aleksandra Pryjda   +3 more
doaj   +1 more source

Investigation of Hydro-Lipophilic Properties of N-Alkoxyphenylhydroxynaphthalenecarboxamides †

Molecules, 2018
The evaluation of the lipophilic characteristics of biologically active agents is indispensable for the rational design of ADMET-tailored structure–activity models.
Iva Kapustikova, Andrzej Bak, Tomas Gonec, Jiri Kos, Violetta Kozik, Josef Jampilek   +5 more
doaj   +1 more source

Assessment of Bioavailability Parameters of Mono- and Bistriazole Derivatives of Propynoylbetulin

Applied Sciences
Bioavailability describes the properties that determine the passage of a compound through biological barriers. In many cases, bioavailability depends on the lipophilicity of the compound.
Monika Kadela-Tomanek, Arkadiusz Sokal, Klaudia Stocerz, Ewa Bębenek, Elwira Chrobak, Paweł Olczyk   +5 more
doaj   +1 more source

The Determination of Partition Coefficient of 6-Mercaptopurine Derivatives by Thin Layer Chromatography

Journal of Chemistry, 2013
Mercaptopurine and its derivatives are used in the treatment of leukemia. To estimate their lipophilicity, a simple and novel thin layer chromatography method was developed. The mobile phase was the mixture of acetonitrile and water.
Andrzej Czyrski, Bartłomiej Kupczyk
doaj   +1 more source

MODELING AND PREDICTION OF AMINO ACIDS LIPOPHYLICITY USING MULTIPLE LINEAR REGRESSION COUPLED WITH GENETIC ALGORITHM

Studia Universitatis Babes-Bolyai Chemia, 2019
Quantitative structure-retention relationships (QSRR) approach was used to model chromatographic lipophilicity of sixteen proteinogenic amino acids using molecular descriptors computed with DRAGON and ALCHEMY software packages.
Alexandrina GUIDEA, Costel SÂRBU
doaj   +1 more source

Transformações Metabólicas de Agrotóxicos em Peixes: Uma Revisão

Orbital: The Electronic Journal of Chemistry, 2016
Fish are among the organisms most damaged by aquatic contamination by pesticides, being ecologically relevant for their bioaccumulation and biomagnification skills of contaminants, which may present health risks to fish consumers.
Ligia Maria Borges Marques Santana, Rivelino Martins Cavalcante   +1 more
doaj   +3 more sources

A novel quinazolinone insulin receptor inhibitor and its synergy with an EGFR inhibitor in glucose‐driven glioblastoma

Molecular Oncology, EarlyView.
The novel styrylquinazolinone‐based molecule W1B effectively suppresses glioblastoma by inhibiting IGF1R and EGFR. In high‐glucose microenvironments driving tumor resistance, W1B acts synergistically with the EGFR inhibitor dacomitinib. This combination safely blocks compensatory survival signaling in zebrafish xenograft models. Showcasing promising in
Patryk Rurka, Wioleta Cieślik, Wojciech Płaziński, Katarzyna Stępnik, Anna Boguszewska‐Czubara, Elżbieta Kot, Robert Musioł, Mateusz Jasica, Anna Mrozek‐Wilczkiewicz, Katarzyna Malarz   +9 more
wiley   +1 more source

Estimation of the octanol-water distribution coefficient of basic compounds by a cationic microemulsion electrokinetic chromatography system

ADMET and DMPK, 2020
The octanol-water partition coefficient (Po/w), or the octanol-water distribution coefficient (Do/w) for ionized compounds, is a key parameter in the drug development process.
Alejandro Fernández-Pumarega, Belén Martín-Sanz, Susana Amézqueta, Elisabet Fuguet, Martí Rosés   +4 more
doaj   +1 more source

Identifying transcription factors controlling the basal expression of human MRP4 highlights a substantial role for Sp1

FEBS Open Bio, EarlyView.
The MRP4 transporter exports several drugs and signaling molecules. Here, we identified key promoter elements regulating basal MRP4 expression. Using reporter assays, we defined a conserved region with essential Sp1 and contributory Ets sites, which controlled basal MRP4 expression.
Debora Singer, Angelique Kragl, Katrin Ziems, Juliane Glaubitz, Sophie Grammbauer, Susanne Hildebrandt, Mladen V. Tzvetkov, Gabriele Jedlitschky   +7 more
wiley   +1 more source

Importin 7 mediates the nuclear import of HIV‐1 integrase via a specific interacting interface

FEBS Open Bio, EarlyView.
HIV‐1 integrase enables viral DNA integration into the host genome. By binding to the core domain of the host protein Importin 7 via its C‐terminal domain, the integrase is transported across the nuclear membrane into the nucleus, where integration of the viral genome into host DNA takes place. This translocation is a critical step for subsequent viral
Juana Bana, Avigail Yariv, Tal Oppenheim, Hadar Amartely, Dana Reichmann, Oded Livnah   +5 more
wiley   +1 more source