23511-93-5Relevant academic research and scientific papers
Synthesis of 4-substituted aminoquinoline-3-carboxylates as potential antimicrobial agents
Marecki,Bambury
, p. 1141 - 1143 (1984)
A series of 4-substituted aminoquinoline-3-carboxylates was prepared and evaluated for antimicrobial activity. Four of the compounds (VIII, XIII, XV, and XXIII) exhibited low activity against Staphylococcus aureus.
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.
