930797-71-0Relevant academic research and scientific papers
Identification of a class of novel tubulin inhibitors
Yi, Xin,Zhong, Bo,Smith, Kerri M.,Geldenhuys, Werner J.,Feng, Ye,Pink, John J.,Dowlati, Afshin,Xu, Yan,Zhou, Aimin,Su, Bin
scheme or table, p. 3425 - 3435 (2012/06/17)
We previously developed a series of anticancer agents based on cyclooxygenase-2 (COX-2) inhibitor nimesulide as a lead compound. However, the molecular targets of these agents still remain unclear. In this study, we synthesized a biotinylated probe based on a representative molecule of the compound library and performed protein pull-down assays to purify the anticancer targets of the compound. Via proteomic approaches, the major proteins bound to the probe were identified to be tubulin and heat shock protein 27 (Hsp27), and the compound inhibited tubulin polymerization by binding at the colchicine domain. However, the tubulin inhibitory effect of the compound activated the Hsp27 phosphorylation and possibly overrode the direct Hsp27 inhibitory effects, which made it difficult to solely validate the Hsp27 target. Taken together, the compound was a dual ligand of tubulin and Hsp27, inhibited tubulin polymerization, and had the potential to be a class of new chemotherapeutic agents.
From COX-2 inhibitor nimesulide to potent anti-cancer agent: Synthesis, in vitro, in vivo and pharmacokinetic evaluation
Zhong, Bo,Cai, Xiaohan,Chennamaneni, Snigdha,Yi, Xin,Liu, Lili,Pink, John J.,Dowlati, Afshin,Xu, Yan,Zhou, Aimin,Su, Bin
, p. 432 - 444 (2012/02/14)
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 ne
AMIDE DERIVATIVES OF BENZENE-SULFONANILIDE, PHARMACEUTICAL COMPOSITION THEREOF AND METHOD FOR CANCER TREATMENT USING THE SAME
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, (2012/04/23)
The invention provides a compound of formula (I), a pharmaceutical composition thereof, a method of preparing a medicament for the treatment of a cancer, and a method of treating cancers. The invention exhibits merits against cancers such as significantly
Design and synthesis of a biotinylated probe of COX-2 inhibitor nimesulide analog JCC76
Zhong, Bo,Lama, Rati,Smith, Kerri M.,Xu, Yan,Su, Bin
scheme or table, p. 5324 - 5327 (2011/10/03)
JCC76 is a derivative of cyclooxygenase-2(COX-2) selective inhibitor nimesulide and exhibits potent anti-breast cancer activity. It selectively induces apoptosis of Her2 positive breast cancer cells. However, the specific molecular targets of JCC76 still
Lead optimization of COX-2 inhibitor nimesulide analogs to overcome aromatase inhibitor resistance in breast cancer cells
Su, Bin,Chen, Shiuan
scheme or table, p. 6733 - 6735 (2010/06/12)
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 aromatas
Synthesis and biological evaluation of selective aromatase expression regulators in breast cancer cells
Su, Bin,Landini, Serena,Davis, Danyetta D.,Brueggemeier, Robert W.
, p. 1635 - 1644 (2007/10/03)
Aromatase converts androgens to estrogens and is a particularly attractive target in the treatment of estrogen receptor positive breast cancer. The enzyme is encoded by the CYP19 gene, which is expressed in a tissue-specific manner. Prostaglandin E2
SULFONANILIDE ANALOGS AS SELECTIVE AROMATASE MODULATORS
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Page/Page column 37; 4/15; 5/15; 12/15, (2010/11/28)
Compounds and methods suppressing aromatase activity expression in cancer cells. Provided are compounds are those of formula I: wherein R1 may be alkyl, cycloakyl, haloalkyl, aryl, substituted aryl, haloaryl, alkoxy, alkylaryl, and arylalkyl; R2 is H, alk
