AI Article Synopsis

  • Lipophilicity is crucial for drug properties, influencing solubility, cell penetration, and transport, which in turn affects pharmacokinetics (ADME).
  • 10-substituted 1,9-diazaphenothiazines exhibit promising anticancer potential by activating mitochondrial apoptosis through the induction of BAX and subsequent caspase activation.
  • The study assessed the lipophilicity of these compounds using theoretical methods and experimental techniques, while also evaluating their pharmacokinetic and toxicological properties, confirming bioavailability through established rules.

Article Abstract

Lipophilicity is one of the key properties of a potential drug that determines the solubility, the ability to penetrate through cell barriers, and transport to the molecular target. It affects pharmacokinetic processes such as adsorption, distribution, metabolism, excretion (ADME). The 10-substituted 1,9-diazaphenothiazines show promising if not impressive in vitro anticancer potential, which is associated with the activation of the mitochondrial apoptosis pathway connected with to induction BAX, forming a channel in MOMP and releasing cytochrome c for the activation of caspases 9 and 3. In this publication, the lipophilicity of previously obtained 1,9-diazaphenothiazines was determined theoretically using various computer programs and experimentally using reverse-phase thin-layer chromatography (RP-TLC) and a standard curve. The study presents other physicochemical, pharmacokinetic, and toxicological properties affecting the bioavailability of the test compounds. ADME analysis was determined in silico using the SwissADME server. Molecular targets studies were identified in silico using the SwissTargetPrediction server. Lipinski's rule of five, Ghose's, and Veber's rules were checked for the tested compounds, confirming their bioavailability.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10138389PMC
http://dx.doi.org/10.3390/ijms24086970DOI Listing

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