三唑基二苯并[]吩嗪可稳定端粒G-四链体并抑制端粒酶。
Triazolyl Dibenzo[]phenazines Stabilize Telomeric G-quadruplex and Inhibit Telomerase.
作者信息
Pal Sarmistha, Fatma Khushnood, Ravichandiran Velayutham, Dash Jyotirmayee
机构信息
School of Chemical Sciences, Indian Association for the Cultivation of Science, Jadavpur, Kolkata-700032, India.
Department of Medicinal Chemistry, NIPER-KOLKATA, Chunilal Bhawan (Adjacent to BCPL), 168, Maniktala Main Road P.O. Bengal Chemicals, P.S. Phoolbagan, Kolkata - 700054, West Bengal.
出版信息
Asian J Org Chem. 2021 Nov;10(11):2921-2926. doi: 10.1002/ajoc.202100468.
We herein report the synthesis and biophysical evaluation of triazolyl dibenzo[]phenazine derivatives as a novel class of G-quadruplex ligands. The aromatic core facilitates π-π interaction and the flexible, protonatable side chains interact with the phosphate backbone of DNA electrostatic interactions. Förster resonance energy transfer (FRET) melting assay and isothermal titration calorimetry (ITC) studies suggest that these ligands show binding preference for the G-quadruplex over G-quadruplexes found in the promoter region of various oncogenes and duplex DNA. The telomeric repeat amplification protocol (Q-TRAP) assay reveals that these ligands reduce telomerase activity in cancer cells.
我们在此报告三唑基二苯并[]吩嗪衍生物作为一类新型G-四链体配体的合成及生物物理评估。芳香核促进π-π相互作用，而柔性的、可质子化的侧链通过静电相互作用与DNA的磷酸骨架相互作用。荧光共振能量转移（FRET）熔解分析和等温滴定量热法（ITC）研究表明，与在各种癌基因启动子区域发现的G-四链体和双链DNA相比，这些配体对G-四链体表现出结合偏好。端粒重复序列扩增协议（Q-TRAP）分析表明，这些配体可降低癌细胞中的端粒酶活性。
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