jcc-76 and nimesulide
jcc-76 has been researched along with nimesulide* in 2 studies
Other Studies
2 other study(ies) available for jcc-76 and nimesulide
| Article | Year |
|---|---|
From COX-2 inhibitor nimesulide to potent anti-cancer agent: synthesis, in vitro, in vivo and pharmacokinetic evaluation.
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 IC(50)s 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 IC(50)s 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. Topics: Animals; Antineoplastic Agents; Benzodioxoles; Cell Line, Tumor; Cell Proliferation; Cyclooxygenase 2; Cyclooxygenase 2 Inhibitors; Drug Design; G1 Phase Cell Cycle Checkpoints; G2 Phase Cell Cycle Checkpoints; Humans; Inhibitory Concentration 50; Male; Mice; Rats; Sulfonamides; Xenograft Model Antitumor Assays | 2012 |
Lead optimization of COX-2 inhibitor nimesulide analogs to overcome aromatase inhibitor resistance in breast cancer cells.
A series of COX-2 selective inhibitor nimesulide derivatives were synthesized. Their anti-cell proliferation activities were evaluated with a long-term estrogen deprived MCF-7aro (LTEDaro) breast cancer cell line, which is the biological model of aromatase inhibitor resistance for hormone-dependent breast cancer. Compared to nimesulide which inhibited LTEDaro cell proliferation with an IC(50) at 170.30 microM, several new compounds showed IC(50) close to 1.0 microM. Topics: Antineoplastic Agents; Aromatase Inhibitors; Breast Neoplasms; Cell Line, Tumor; Cell Proliferation; Cyclooxygenase 2 Inhibitors; Dose-Response Relationship, Drug; Drug Resistance, Neoplasm; Drug Screening Assays, Antitumor; Humans; Molecular Structure; Stereoisomerism; Structure-Activity Relationship; Sulfonamides | 2009 |