Nanomolar Selective G Quadruplex Ligands from One Pot Thermodynamic and Structural Studies of Azacyanines

Date

2008-11-15

Author

Engelhart, Aaron
Persil Çetinkol, Özgül
Nanjunda, Rupesh
Wılson, Davıd
Hud, Nıcholas

Metadata

Show full item record

Item Usage Stats

151
views

0
downloads

The observation that G-quadruplex structures exist in nucleic acid sequences associated with cancers has generated substantial interest in G quadruplexes as potential antineoplastics. The G quadruplex, with planar G tetrads, is an appealing nucleic acid drug target, as the G tetrad is structurally distinct from the Watson-Crick base pair. High-affinity G-quadruplex ligands have begun to show medicinal promise, although the connection between G-quadruplex binding and in vivo activity might not always be obvious. Here, we report a novel, high-affinity, high-selectivity scaffold for G-quadruplex ligands: the azacyanines. We present data on the G-quadruplex and Watson-Crick dsDNA binding affinity of these ligands. Additionally, we present data related to the binding site for these ligands on the G quadruplex formed by the human telomeric DNA repeat in potassium solution.

URI

https://hdl.handle.net/11511/79644

Conference Name

Southeast Regional Meeting of the ACS (2008)

Collections

Department of Chemistry, Conference / Seminar

Suggestions

OpenMETU
Core

Chemoenzymatic synthesis of chiral hydroxymethyl cycloalkenols Şenocak, Deniz; Demir, Ayhan Sıtkı; Department of Chemistry (2004) Chiral cyclic alkenols with hydroxymethyl functionality are important structural units in many biologically active natural compouds such as prostaglandins, sesquiterpene antiviral agents, pentenomycins, xanthocidin, sarkomycin, etc. 1,3-cycloalkanediones are converted into bicyclic polyoxo derivatives with formaldehyde and trioxane in the presence of Lewis acid. Selective oxidation of the bicyclic compounds by using manganese(III)acetate followed by enzyme-catalyzed kinetic resolution afforded chiral bicycl...
Enantioselective Friedel-Crafts alkylation of indole with nitroalkenes in the presence of bifunctional squaramide organocatalysts Dündar, Esra; Tanyeli, Cihangir (2021-01-01) A series of chiral bifunctional quinine and 2-aminoDMAP based squaramide organocatalysts are evaluated in Friedel-Crafts alkylation of indoles with nitroolefins. These 3-substituted indole derivatives are synthesized in the presence of sterically encumbered tert-butyl squaramide/quinine with high enantioselectivity (up to >99% ee) and moderate chemical yields (up to 80%) by representing as chiral precursors for very important biologically active molecules. Besides, this asymmetric transformation provides a ...
Dimethyl ether, diethyl ether & ethylene from alcohols over tungstophosphoric acid based mesoporous catalysts Ciftci, Aysegul; VARIŞLI, DİLEK; Tokay, Kenan Cem; Sezgi, Naime Aslı; Doğu, Timur (2012-10-01) Tungstophosphoric acid (TPA) incorporated silicate structured new mesoporous catalysts were synthesized following one-pot hydrothermal and impregnation procedures. Surface area of TPA@MCM-41, which was prepared by impregnating TPA into MCM-41, was two orders of magnitude higher than the surface area of pure TPA and this catalyst showed very high activity in dehydration reactions of both ethanol and methanol. Ethanol fractional conversion values reaching to 1.0 was obtained at 300 degrees C at a space time o...
NANOSCALE FLUID-STRUCTURE INTERACTIONS IN CYTOPLASM DURING FREEZING Özçelikkale, Altuğ (2013-01-01) In this study, a theoretical model is developed to simulate the biophysical events in the intracellular spaces considering the biphasic, i.e., poroelastic, behavior of the cytoplasm. Most previous studies in the cryobiology literature have modeled the biophysical response of cells to freezing assuming the spatial homogeneity of all physical properties within the intracellular space without considering fluid-structure interaction in both the intracellular and extracellular spaces. However, a few recent studi...
Facile synthesis of (4-nitrophenyl)thio-substituted 1- pyrrolines Korkmaz, Esra; Zora, Metin; Department of Chemistry (2019) The importance of heterocyclic compounds is enormous in synthetic organic chemistry due to their presence in bioactive molecules. Five-membered 1-pyrrolines are one of the most important classes of them. They have recently drawn great attention from synthetic chemists since they have a prominent role for the synthesis of a great number of pharmaceutical molecules. Therefore, there is intense research on their synthesis. In this project, we concentrated on the synthesis of (4-nitrophenyl)thio-substituted 1- ...

Citation Formats

A. Engelhart, Ö. Persil Çetinkol, R. Nanjunda, D. Wılson, and N. Hud, “Nanomolar Selective G Quadruplex Ligands from One Pot Thermodynamic and Structural Studies of Azacyanines,” presented at the Southeast Regional Meeting of the ACS (2008), 2008, Accessed: 00, 2021. [Online]. Available: https://hdl.handle.net/11511/79644.