Department of Chemistry, College of Sciences and Health Professions, Cleveland State University, 2121 Euclid Ave., Cleveland, OH 44115, USA.
Bioorg Med Chem Lett. 2011 Sep 15;21(18):5324-7. doi: 10.1016/j.bmcl.2011.07.025. Epub 2011 Jul 14.
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 remain unclear, which significantly withdraw the further drug development of JCC76. To identify the molecular targets of JCC76, a six carbon linker and biotin conjugated JCC76 probe was designed and synthesized. The anti-proliferation activity of the probe and its analogs was evaluated.
JCC76 是环氧化酶-2（COX-2）选择性抑制剂尼美舒利的衍生物，具有很强的抗乳腺癌活性。它选择性地诱导 Her2 阳性乳腺癌细胞凋亡。然而，JCC76 的具体分子靶点仍不清楚，这极大地阻碍了 JCC76 的进一步药物开发。为了确定 JCC76 的分子靶点，设计并合成了一个带有 6 个碳链接子和生物素的 JCC76 探针。评估了探针及其类似物的抗增殖活性。
