66490-31-1

Usage

Uses

Used in Pharmaceutical Industry:
4-Chloro-3-methylbenzo[b]thiophene-2-carboxylic acid is used as a pharmaceutical intermediate for the development of new drugs. Its unique structural features and potential to interact with biological targets make it a promising candidate for the treatment of various diseases.
Used in Organic Synthesis:
4-Chloro-3-methylbenzo[b]thiophene-2-carboxylic acid is used as a building block for the synthesis of other organic compounds with desirable properties. Its versatility in chemical reactions allows for the creation of a wide range of molecules with potential applications in various industries.
Used in Chemical Research:
4-Chloro-3-methylbenzo[b]thiophene-2-carboxylic acid is used as a subject of study in chemical research. Its unique structural features and potential applications make it an interesting target for further investigation and development.

Upstream product

• 87327-69-3 1-(2-chloro-6-fluorophenyl)ethan-1-one 
• 1415968-73-8 methyl 4-chloro-3-methylbenzo[b]thiophene-2-carboxylate 

Downstream Products

• 1415968-54-5 4-chloro-3-(3-(4-chloro-3,5-dimethylphenoxy)propyl)benzo[b]thiophene-2-carboxylic acid 

Relevant academic research and scientific papers

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.

Discovery of potent myeloid cell leukemia 1 (Mcl-1) inhibitors using fragment-based methods and structure-based design

Myeloid cell leukemia 1 (Mcl-1), a member of the Bcl-2 family of proteins, is overexpressed and amplified in various cancers and promotes the aberrant survival of tumor cells that otherwise would undergo apoptosis. Here we describe the discovery of potent and selective Mcl-1 inhibitors using fragment-based methods and structure-based design. NMR-based screening of a large fragment library identified two chemically distinct hit series that bind to different sites on Mcl-1. Members of the two fragment classes were merged together to produce lead compounds that bind to Mcl-1 with a dissociation constant of 100 nM with selectivity for Mcl-1 over Bcl-xL and Bcl-2. Structures of merged compounds when complexed to Mcl-1 were obtained by X-ray crystallography and provide detailed information about the molecular recognition of small-molecule ligands binding Mcl-1. The compounds represent starting points for the discovery of clinically useful Mcl-1 inhibitors for the treatment of a wide variety of cancers.