Document Type
Article
Publication Date
1-1-2012
Publication Title
European Journal of Medicinal Chemistry
Abstract
Cyclooxygenase-2 (COX-2) inhibitor nimesulide inhibits the proliferation of various types of cancer cells mainly via COX-2 independent mechanisms, which makes it a good lead compound for anti-cancer drug development. In the presented study, a series of new nimesulide analogs were synthesized based on the structure–function analysis generated previously. Some of them displayed very potent anti-cancer activity with IC50s around 100 nM–200 nM to inhibit SKBR-3 breast cancer cell growth. CSUOH0901 (NSC751382) from the compound library also inhibits the growth of the 60 cancer cell lines used at National Cancer Institute Developmental therapeutics Program (NCIDTP) with IC50s around 100 nM–500 nM. Intraperitoneal injection with a dosage of 5 mg/kg/d of CSUOH0901 to nude mice suppresses HT29 colorectal xenograft growth. Pharmacokinetic studies demonstrate the good bioavailability of the compound.
Recommended Citation
Zhong, Bo; Cai, Xiaohan; Chennamaneni, Snigdha; Yi, Xin; Liu, Lili; Pink, John J.; Dowlati, Afshin; Xu, Yan; Zhou, Aimin; and Su, Bin, "From COX-2 Inhibitor Nimesulide to Potent Anti-Cancer Agent: Synthesis, In Vitro, In Vivo and Pharmacokinetic Evaluation" (2012). Chemistry Faculty Publications. 196.
https://engagedscholarship.csuohio.edu/scichem_facpub/196
Creative Commons License
This work is licensed under a Creative Commons Attribution-Noncommercial-No Derivative Works 3.0 License.
DOI
10.1016/j.ejmech.2011.11.012
Version
Postprint
Volume
47
