1620232-95-2Relevant academic research and scientific papers
A kind of acridine compounds and use thereof
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, (2016/11/21)
The invention provides an acridine compound and an application thereof. The compound has a structure as shown in a general formula I described in the specification, wherein R1 is selected from H or -CO-Ph-(o,m,p) R4; R2 is selected from O or -N-Ph-(o,m,p)
Two-face, two-turn α-helix mimetics based on a cross-acridine scaffold: Analogues of the bim BH3 domain
Li, Xiangqian,Wang, Ziqian,Feng, Yingang,Song, Ting,Su, Pengchen,Chen, Chengbin,Chai, Gaobo,Yang, Ying,Zhang, Zhichao
, p. 1280 - 1285 (2014/06/24)
The design of a cross-acridine scaffold mimicking the i, i+3, i+5, and i+7 residues distributed over a two-face, two-turn α-helix is described. Docking studies and 2D 1H,15N HSQC NMR spectroscopy provide compelling evidence that compound 3-d accurately reproduces the arrangement of four hotspots in the Bim BH3 peptide to permit binding to the Mcl-1 and Bcl-2 proteins (Ki 0.079 and 0.056 μM, respectively). Furthermore, the hotspot mutation could also be mimicked by individual or multiple deletions of side chains on the scaffold. Building site: A cross-acridine scaffold was designed to project functional groups with spatial and angular geometries that accurately mimic the i, i+3, i+5, and i+7 side chains on a two-turn, two-face section of an α-helix. The binding mode of the most potent compound, 3-d, to Mcl-1 was confirmed by 1H, 15N HSQC NMR.
