26583-62-0

Upstream product

• 106-93-4 ethylene dibromide 
• 58962-45-1 Potassium; 4-chloro-3,5-dimethyl-phenolate 
• 88-04-0 4-Chloro-3,5-dimethylphenol 

Downstream Products

• 68381-56-6 2-[2-(4-Chloro-3,5-dimethyl-phenoxy)-ethylsulfanyl]-succinic acid diethyl ester 
• 68381-62-4 2-[2-(4-Chloro-3,5-dimethyl-phenoxy)-ethylsulfanyl]-butane-1,4-diol 
• 68381-69-1 2-[2-(4-Chloro-3,5-dimethyl-phenoxy)-ethanesulfonyl]-butane-1,4-diol 
• 68381-76-0 Methanesulfonic acid 2-[2-(4-chloro-3,5-dimethyl-phenoxy)-ethanesulfonyl]-4-methanesulfonyloxy-butyl ester 
• 1415968-53-4 3-(3-(4-chloro-3,5-dimethylphenoxy)propyl)benzo[b]thiophene-2-carboxylic acid 
• 1415968-60-3 3-(3-(4-chloro-3,5-dimethylphenoxy)propyl)benzofuran-2-carboxylic acid 

Relevant academic research and scientific papers

Discovery and structure-activity relationship studies of N-substituted indole derivatives as novel Mcl-1 inhibitors

Myeloid cell leukemia-1 (Mcl-1) is an important antiapoptotic protein functioning through protein-protein interactions. We discovered LSL-A6 (2-((2-carbamoyl-1-(3-(4-methoxyphenoxy)propyl)-1H-indol-6-yl)oxy)acetic acid) with a novel N-substituted indole scaffold to interfere Mcl-1 binding as a novel Mcl-1 inhibitor. Molecular modeling indicated that this compound binds with Mcl-1 by interaction with P2 and R263 hot-spots. Structure modification focused on several moieties including indole core, hydrophobic tail and acidic chain were conducted and structure-activity relationship was analyzed. The most potent compound 24d which exhibited Ki value of 110?nM for interfering Mcl-1 binding was obtained after hit-to-lead modification.

SUBSTITUTED BENZOFURAN, BENZOTHIOPHENE AND INDOLE MCL-1 INHIBITORS

The present invention provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein.