Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Cancer

Cancer

Topoisomerase I (TOP1)

In vitro and mouse studies suggest fluorinated camptothecin could be used to treat cancer. a-Fluoroether-modified camptothecins had greater stability in phosphate buffered saline than unmodified camptothecin and maintained inhibitory activity against TOP1. In human lung, breast and colon cancer cells, the fluorinated camptothecins decreased proliferation compared with vehicle. In mouse xenograft models of human lung cancer, one of the compounds had antitumor activity comparable to that of the camptothecin topotecan. Next steps include optimizing a clinical candidate from the series.

SciBX 6(43); doi:10.1038/scibx.2013.1219
Published online Nov. 7, 2013

Patent application filed; available for licensing

Miao, Z. et al. J. Med. Chem.; published online Sept. 26, 2013;
doi:10.1021/jm400906z
Contact: Wannian Zhang, Second Military Medical University,
Shanghai, China
e-mail:

zhangwnk@hotmail.com
Contact: Chunquan Sheng, same affiliation as above
e-mail:

shengcq@hotmail.com
Contact: Zhenyuan Miao, same affiliation as above
e-mail:

miaozhenyuan@hotmail.com