473225-47-7Relevant academic research and scientific papers
Nontoxic combretafuranone analogues with high in vitro antibacterial activity
Horky,Vorá?ová,Kone?ná,Sedlák,Bart?něk,Vacek,Kune?,Pour
, p. 843 - 853 (2017/12/13)
A library of thirty two 3,4-diphenylfuranones related to both combretastatin A-4 and antifungal 5-(acyloxymethyl)-3-(halophenyl)-2,5-dihydrofuran-2-ones was prepared. Cytotoxic effects on a panel of cancer and normal cell lines and antiinfective activity
Design of fluorine-containing 3,4-diarylfuran-2(5H)-ones as selective COX-1 inhibitors
Uddin, Md. Jashim,Elleman, Anna V.,Ghebreselasie, Kebreab,Daniel, Cristina K.,Crews, Brenda C.,Nance, Kellie D.,Huda, Tamanna,Marnett, Lawrence J.
supporting information, p. 1254 - 1258 (2015/04/27)
We report the design and synthesis of fluorine-containing cyclooxygenase-1 (COX-1)-selective inhibitors to serve as prototypes for the development of a COX-1-targeted imaging agent. Deletion of the SO2CH3 group of rofecoxib switches the compound from a COX-2- to a COX-1-selective inhibitor, providing a 3,4-diarylfuran-2(5H)-one scaffold for structure-activity relationship studies of COX-1 inhibition. A wide range of fluorine-containing 3,4-diarylfuran-2(5H)-ones were designed, synthesized, and tested for their ability to selectively inhibit COX-1 in purified protein and human cancer cell assays. Compounds containing a fluoro-substituent on the C-3 phenyl ring and a methoxy-substituent on the C-4 phenyl ring of the 3,4-diarylfuran-2(5H)-one scaffold were the best COX-1-selective agents of those evaluated, exhibiting IC50s in the submicromolar range. These compounds provide the foundation for development of an agent to facilitate radiologic imaging of ovarian cancer expressing elevated levels of COX-1.
Design and Synthesis of Novel Rofecoxib Analogs as Potential Cyclooxygenase (COX-2) Inhibitors: Replacement of the Methylsulfonyl Pharmacophore by a Sulfonylazide Bioisostere
Uddin, Md. Jashim,Rao, P.N. Praveen,Knaus, Edward E.
, p. 861 - 868 (2007/10/03)
A group of rofecoxib analogs, having a sulfonylazide (SO2N 3) substituent in place of the methanesulfonyl (SO2CH 3) pharmacophore at the meta-position viz 3-(4-methyl, 4-methoxy, or 4-ethoxyphenyl)-4-(3-sulfonyl
