New quinazoline derivatives for telomeric G-quadruplex DNA: effects of an added phenyl group on quadruplex binding ability.
New quinazoline derivatives for telomeric G-quadruplex DNA: effects of an added phenyl group on quadruplex binding ability.
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DOI:
10.1016/j.ejmech.2013.01.051
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发表时间:
2013-05
影响因子:
6.7
通讯作者:
Jin-Hui He;Hui-Yun Liu;Zeng Li;Jia-Heng Tan;Tian-Miao Ou;Shi-Liang Huang;Lin-Kun An;Ding Li;L. Gu;Zhishu Huang
中科院分区:
文献类型:
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作者:
Jin-Hui He;Hui-Yun Liu;Zeng Li;Jia-Heng Tan;Tian-Miao Ou;Shi-Liang Huang;Lin-Kun An;Ding Li;L. Gu;Zhishu Huang
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.