1448458-77-2Relevant articles and documents
Rofecoxib-like derivative, prepared organic fluorescent dye skeleton and application
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Paragraph 0055-0059; 0060-0062, (2021/02/10)
The invention belongs to the technical field of biomedical materials, particularly relates to a rofecoxib-like derivative, and further discloses an organic fluorescent dye skeleton prepared from the rofecoxib-like derivative and application of the rofecoxib-like derivative in the field of biological imaging. According to the rofecoxib-like series derivative disclosed by the invention, one-step condensation modification is only carried out on the basis of a COX-2 inhibitor rofecoxib structure through a computational chemistry and quantum orbital theory speculation technology, and a plurality ofsmall molecular fluorescent dyes and COX-2 inhibitor fluorescent probes with clinical development prospects are synthesized by adopting a brand-new design strategy; on the basis of keeping the strongCOX-2 enzyme inhibition activity, the photophysical and photochemical properties of the fluorescent dye are effectively improved, the fluorescent dye shows excellent fluorescence properties, and a more ideal choice is provided for the design of the fluorescent dye and the probe in the future.
Stereoselective synthesis and anti-proliferative effects on prostate cancer evaluation of 5-substituted-3,4-diphenylfuran-2-ones
Liu, Gai-Zhi,Xu, Hai-Wei,Wang, Peng,Lin, Zong-Tao,Duan, Ying-Chao,Zheng, Jia-Xin,Liu, Hong-Min
, p. 323 - 336 (2013/10/01)
Series of 5-substituted-3,4-diphenylfuran-2-ones were stereoselectively prepared. Their potential anti-proliferative effects on prostate cancer and some of their cyclooxygenases (COXs) inhibitory activities were evaluated. Structure-activity relationship (SAR) data, acquired by substituent modification at the para-position and ortho-position of the C-3 phenyl ring and 5-substituted modification of the central furanone, showed that 3-(2-chloro-phenyl)-4-(4-methanesulfonyl-phenyl)-5-(1-methoxy-ethyl) -5H-furan-2-one (13p) was the most potent compound and could effectively reduce the proliferation of prostate cancer cells (PC3 cell IC50 = 20 μM; PC3 PCDNA cell IC50 = 5 μM; PC3 SKP2 cell IC50 = 5 μM; DU145 cell IC50 = 25 μM). The cell cycle analysis for 13p in DU145 indicated that 13p may induce G1 phase arrest.