1616557-72-2

Upstream product

• 1616558-01-0 C₂₆H₂₆ClNO₂S 
• 1616558-09-8 C₁₇H₁₈ClNS 
• 1616557-98-2 C₂₂H₂₆ClNO₂S 
• 1027143-39-0 4-(2-bromo-phenylsulfanyl)-piperidine-1-carboxylic acid tert-butyl ester 
• 6320-02-1 o-bromothiophenol 
• 180695-79-8 tert-butyl 4-bromo-1-piperidinecarboxylate 
• 1027345-12-5 [4-((R)-3-morpholin-4-yl-1-phenylsulfanyl-methyl-propylamino)-3-trifluoromethanesulfonyl]benzenesulfonamide 
• 1616558-12-3 C₂₄H₂₂ClNO₃S 
• 1627704-47-5 C₂₆H₂₆ClNO₃S 

Relevant academic research and scientific papers

Towards the next generation of dual Bcl-2/Bcl-xL inhibitors

Structural modifications of the left-hand side of compound 1 were identified which retained or improved potent binding to Bcl-2 and Bcl-x L in in vitro biochemical assays and had strong activity in an RS4;11 apoptotic cellular assay. For example, sulfoxide diastereomer 13 maintained good binding affinity and comparable cellular potency to 1 while improving aqueous solubility. The corresponding diastereomer (14) was significantly less potent in the cell, and docking studies suggest that this is due to a stereochemical preference for the RS versus SS sulfoxide. Appending a dimethylaminoethoxy side chain (27) adjacent to the benzylic position of the biphenyl moiety of 1 improved cellular activity by approximately three-fold, and this activity was corroborated in cell lines overexpressing Bcl-2 and Bcl-xL.