Journal ArticleDOI
Xanthone Derivatives as potential Telomeric G-Quadruplex Stabilizing and Cytotoxic Agents: Effects of Substitution on Quadruplex Binding Affinity and Cytotoxicity
TLDR
A series of xanthone derivatives (2a-2e) as telomeric quadruplex stabilizing ligands were designed, synthesized and evaluated by molecular docking, drug-likeness prediction, spectroscopy assay, melting profiles, PCR stop analysis as mentioned in this paper .About:
This article is published in Journal of Molecular Structure.The article was published on 2022-08-01. It has received 2 citations till now. The article focuses on the topics: Chemistry & Cytotoxicity.read more
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Design and Synthesis of Xanthone Analogues Conjugated with Aza‐aromatic Substituents as Promising G‐Quadruplex Stabilizing Ligands and their Selective Cancer Cell Cytotoxic Action
TL;DR: In this article , the authors examined the stabilization of higher-order noncanonical Gquadruplex (G4) DNA structures formed by the Grich sequences in the promoter region of oncogenes such as c−MYC, c−KIT, VEGF and BCl2 by newly synthesized, novel nitrogen-containing aromatics conjugated to xanthone moiety.
References
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Apoptosis: A Review of Programmed Cell Death
TL;DR: The goal of this review is to provide a general overview of current knowledge on the process of apoptosis including morphology, biochemistry, the role of apoptoses in health and disease, detection methods, as well as a discussion of potential alternative forms of apoptotic proteins.
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Crystal structure of parallel quadruplexes from human telomeric DNA.
TL;DR: This crystal structure of a quadruplex formed from four consecutive human telomeric DNA repeats and grown at a K+ concentration that approximates its intracellular concentration suggests a straightforward path for telomere folding and unfolding, as well as ways in which it can recognize telomerre-associated proteins.
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A bioavailability score.
TL;DR: This work has developed a score that assigns the probability that a compound will have F > 10% in the rat, and distinguishes compounds that are poorly permeable from those that are permeable in Caco-2 cells.
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The G-quadruplex-interactive molecule BRACO-19 inhibits tumor growth, consistent with telomere targeting and interference with telomerase function.
Angelika M. Burger,Fangping Dai,Christoph Schultes,Anthony P. Reszka,Michael J. Moore,John A. Double,Stephen Neidle +6 more
TL;DR: The in vitro and in vivo data presented here is consistent with the G-quadruplex binding ligand BRACO-19 producing an anticancer effect by inhibiting the capping and catalytic functions of telomerase.
Journal ArticleDOI
Computational methods for the prediction of 'drug-likeness'
TL;DR: The authors examine the growing role that is being played by computational methods in this filtering process, with a particular focus on the prediction of intestinal absorption and blood-brain barrier penetration.