Document Type
Article
Publication Date
9-1-2012
Publication Title
Bioorganic & Medicinal Chemistry Letters
Abstract
The potency of a series of sulfonamide tubulin inhibitors against the growth of Trypanosoma brucei (T. brucei), as well as human cancer and primary fibroblast cells were evaluated with the aim of determining whether compounds that selectively inhibit parasite proliferation could be identified. Several compounds showed excellent selectivity against T. brucei growth, and have the potential to be used for the treatment of Human African trypanosomiasis. A T. brucei tubulin protein homology model was built based on the crystal structure of the bovine tubulin. The colchicine-binding domain, which is also the binding site of the tested sulfonamide tubulin inhibitors, showed clear differences between the tubulin structures and presumably explained the selectivity of the compounds.
Recommended Citation
Lama, Rati; Sandhu, Ranjodh; Zhong, Bo; Li, Bibo; and Su, Bin, "Identification of Selective Tubulin Inhibitors as Potential Anti-Trypanosomal Agents" (2012). Chemistry Faculty Publications. 393.
https://engagedscholarship.csuohio.edu/scichem_facpub/393
Creative Commons License
This work is licensed under a Creative Commons Attribution-NonCommercial-No Derivative Works 4.0 International License.
DOI
10.1016/j.bmcl.2012.07.023
Version
Postprint
Volume
22
Issue
17
Comments
This work was supported by National Institutes of Health R01 Grant AI066095 (B.L. as PI) and the startup fund from CSU (B.S. as PI).