Targeting FtsZ for antituberculosis drug discovery: noncytotoxic taxanes as novel antituberculosis agents.

@article{Huang2006TargetingFF,
  title={Targeting FtsZ for antituberculosis drug discovery: noncytotoxic taxanes as novel antituberculosis agents.},
  author={Qing Huang and Fumiko Kirikae and Teruo Kirikae and Antonella Pepe and Amol G Amin and Laurel Respicio and Richard A. Slayden and Peter J. Tonge and Iwao Ojima},
  journal={Journal of medicinal chemistry},
  year={2006},
  volume={49 2},
  pages={463-6}
}
Screening of 120 taxanes identified a number of compounds that exhibited significant antituberculosis activity. Rational optimization of selected compounds led to the discovery that the C-seco-taxane-multidrug-resistance (MDR) reversal agents (C-seco-TRAs) are noncytotoxic at the upper limit of solubility and detection (>80 microM), while maintaining MIC(99) values of 1.25-2.5 microM against drug-resistant and drug-sensitive strains of Mycobacterium tuberculosis (MTB). Treatment of MTB cells… CONTINUE READING

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