1083313-76-1Relevant articles and documents
Synthesis and antibacterial activity of novel ketolides with 11,12-quinoylalkyl side chains
Zhao, Zhe-hui,Zhang, Xiao-xi,Jin, Long-long,Yang, Shuang,Lei, Ping-sheng
, p. 2358 - 2363 (2018)
A series of quinoylalkyl side chains was designed and synthesized, followed by introduction into ketolides by coupling with building block 6 or 32. The corresponding targets 7a–n, 33b, and 33e were tested for their in vitro activities against a series of macrolide-sensitive and macrolide-resistant pathogens. Some of them showed a similar antibacterial spectrum and comparable activity to telithromycin. Among them, two C2-F ketolides, compounds 33b and 33e, displayed excellent activities against macrolide-sensitive and macrolide-resistant pathogens.
The design, synthesis, and evaluation of coumarin ring derivatives of the novobiocin scaffold that exhibit antiproliferative activity
Donnelly, Alison C.,Mays, Jared R.,Burlison, Joseph A.,Nelson, John T.,Vielhauer, George,Holzbeierlein, Jeffrey,Blagg, Brian S. J.
experimental part, p. 8901 - 8920 (2009/04/11)
(Chemical Equation Presented) Novobiocin, a known DNA gyrase inhibitor, binds to a nucleotide-binding site located on the Hsp90 C-terminus and induces degradation of Hsp90-dependent client proteins at ～700 μM in breast cancer cells (SKBr3). Although many analogues of novobiocin have been synthesized, it was only recently demonstrated that monomeric species exhibit antiproliferative activity against various cancer cell lines. To further refine the essential elements of the coumarin core, a series of modified coumarin derivatives was synthesized and evaluated to elucidate structure-activity relationships for novobiocin as an anticancer agent. Results obtained from these studies have produced novobiocin analogues that manifest low micromolar activity against several cancer cell lines.
