Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 63, Issue -, Pages 1-13Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.01.051
Keywords
Quinazoline derivatives; Telomeric G-quadruplex DNA; Inducing ability; Telomerase inhibitor; Telomere shortening
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Funding
- Natural Science Foundation of China [91213302, 21172272, 81001400]
- International S&T Cooperation Program of China [2010DFA34630]
- Science Foundation of Guangzhou [2009A1-E011-6]
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To improve the selectivity of indoloquinoline or benzofuroquinoline derivatives, we previously reported several quinazoline derivatives [17]. These compounds could mimic a tetracyclic aromatic system through intramolecular hydrogen bond. Studies showed that these quinazoline derivatives were effective and selective telomeric G-quadruplex ligands. With this encouragement, here we synthesized a series of N-(2-(quinazolin-2-yl)phenyl)benzamide (QPB) compounds as modified quinazoline derivatives. In this modification, a phenyl group was introduced to the aromatic core. The evaluation results showed that part of QPB derivatives had stronger binding ability and better selectivity for telomeric G-quadruplex DNA than LZ-11, the most potential compound of reported quinazoline derivatives. Furthermore, telomerase inhibition of QPB derivatives and their cellular effects were studied. (c) 2013 Elsevier Masson SAS. All rights reserved.
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