108138-27-8Relevant articles and documents
Synthesis, molecular docking and biological evaluation of quinolone derivatives as novel anticancer agents
Li, Jie,Zheng, Tu-Cai,Jin, Yi,Xu, Jian-Guo,Yu, Jian-Gang,Lv, Yan-Wen
, p. 55 - 60 (2018)
A series of novel quinolone derivatives (8a-j) were synthesized, and their anticancer activities were tested in human cancer cell lines, human lung carcinoma cell (A549), human promyelocytic leukemia cell (HL-60), and human cervical cancer cell (Hela). Compound 8i was found to be 5-times more potent in cellkilling activity for cell lines A549, HL-60, and Hela than the positive control irinotecan or cisplatin, with IC50 of 0.009, 0.008 and 0.010 μM, respectively. The docking study revealed that compound 8i might have strong interactions with the active site of DNA-topoisomerase I.
Effect of Lipophilicity at N-1 on Activity of Fluoroquinolones against Mycobacteria
Renau, Thomas E.,Sanchez, Joseph P.,Shapiro, Martin A.,Dever, Julie A.,Gracheck, Stephen J.,Domagala, John M.
, p. 2974 - 2977 (2007/10/02)
The dramatic increase in drug resistant Mycobacterium tuberculosis has caused a resurgence in research targeted toward these organisms.As part of a systematic study to optimize the quinolone antibacterials against mycobacteria, we have prepared a series of N-1-phenyl-substituted derivatives to explore the effect of increasing lipophilicity on potency at this position.The compounds, synthesized by the modification of a literature procedure, were evaluated for activity against Gram-negative and Gram-positive bacteria, Mycobacterium fortuitum and Mycobacterium smegmatis, and the results correlated with log P, pKa, and other attributes.The activity of the compounds against the rapidly growing, less hazardous organism M. fortuitum was used as a measure of M. tuberculosis activity.The results demonstrate that increasing lipophilic character by itself does not correlate with increased potency against mycobacteria.Rather, intrinsic activity against Gram-negative and/or Gram-positive bacteria is the governing factor for corresponding activity against mycobacteria.