226398-85-2

Upstream product

• 226389-21-5 4-[(4-fluorophenyl)sulfonyl]tetrahydro-N-[(tetrahydro-2H-pyran-2-yl)oxy]-2H-pyran-4-carboxamide 
• 106-48-9 4-chloro-phenol 
• 226396-71-0 2-(4-fluorobenzenesulfonyl)acetic acid methyl ester 
• 226396-70-9 (4-fluoro-phenylsulfanyl)-acetic acid methyl ester 
• 371-42-6 4-Fluorothiophenol 
• 226396-72-1 4-(4-fluoro-benzenesulfonyl)-tetrahydro-pyran-4-carboxylic acid methyl ester 
• 226398-02-3 4-(4-fluoro-benzenesulfonyl)-tetrahydro-pyran-4-carboxylic acid 

Relevant academic research and scientific papers

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl Sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease

α-Sulfone-α-piperidine and α-tetrahydropyranyl hydroxamates were explored that are potent inhibitors of MMPs-2,-9, and-13 that spare MMP-1, with oral efficacy in inhibiting tumor growth in mice and left-ventricular hypertrophy in rats and in the bovine cartilage degradation ex vivo explant system. α-Piperidine 19v (SC-78080/SD-2590) was selected for development toward the initial indication of cancer, while α-piperidine and α-tetrahydropyranyl hydroxamates 19w (SC-77964) and 9i (SC-77774), respectively, were identified as backup compounds.

Synthesis and structure-activity relationships of β- and α-piperidine sulfone hydroxamic acid matrix metalloproteinase inhibitors with oral antitumor efficacy

α-Piperidine-β-sulfone hydroxamate derivatives were explored that are potent for matrix metalloproteinases (MMP)-2, -9, and -13 and are sparing of MMP-1. The investigation of the β-sulfones subsequently led to the discovery of hitherto unknown α-sulfone h