916204-05-2

Usage

Uses

Used in Pharmaceutical Industry:
4-[4-(4'-Chlorobiphenyl-2-ylmethyl)piperazin-1-yl]benzoic Acid is used as a chemical intermediate for the synthesis of ABT 737, a potent Bcl-2 family inhibitor. 4-[4-(4'-Chlorobiphenyl-2-ylmethyl)piperazin-1-yl]benzoic Acid is instrumental in the development of targeted therapies for small cell lung cancer, as ABT-737 has been shown to induce dramatic regressions in tumors derived from some SCLC cell lines. Its role in the production of ABT 737 highlights its importance in advancing cancer treatment options.

Upstream product

• 451-46-7 4-fluorobenzoic acid ethyl ester 
• 1679-18-1 4-Chlorophenylboronic acid 
• 1001754-57-9 2-bromomethyl-4'-chlorobiphenyl 
• 773872-47-2 (4′-chloro-[1,1′-biphenyl]-2-yl)methanol 
• 6630-33-7 ortho-bromobenzaldehyde 
• 80518-57-6 ethyl 4-(piperazin-1-yl)benzoate 
• 926934-01-2 4-[4-(2-bromo-benzyl)-piperazin-1-yl]-benzoic acid ethyl ester 
• 926934-07-8 4-[4-(4'-chloro-biphenyl-2-ylmethyl)-piperazin-1-yl]-benzoic acid ethyl ester 

Downstream Products

• 1012060-01-3 (R)-ethyl 2-((3-(4-(N-(4-(4-((4'-chlorobiphenyl-2-yl)methyl)piperazin-1-yl)benzoyl)sulfamoyl)-2-nitrophenylamino)-4-(phenylthio)butyl)(methyl)amino)acetate 
• 852808-13-0 (R)-4-(4-((4'-chlorobiphenyl-2-yl)methyl)piperazin-1-yl)-N-(3-nitro-4-(2-(phenylthio)ethylamino)phenylsulfonyl)benzamide 
• 852808-14-1 (R)-4-(4-((4'-chlorobiphenyl)methyl)piperazin-1-yl)-N-(4-(4-morpholino-1-(phenylthio)butan-2-ylamino)-3-nitrophenylsulfonyl)benzamide 
• 1065603-44-2 (R)-4-(-4-((4'-chlorobiphenyl-2-yl)methyl)piperazin-1-yl)-N-(4-(4-(dimethylamino)-1-(phenylthio)butan-2-ylamino)-3-(2,2,2-trifluoroacetyl)phenylsulfonyl)benzamide 
• 920516-38-7 (R)-4-(-4-((4'-chlorobiphenyl-2-yl)methyl)piperazin-1-yl)-N-(4-(4-(dimethylamino)-1-(phenylthio)butan-2-ylamino)-3-(methylsulfonyl)phenylsulfonyl)benzamide 
• 852809-06-4 (R)-4-(-4-((4'-chlorobiphenyl-2-yl)methyl)piperazin-1-yl)-N-(3-cyano-4-(4-(dimethylamino)-1-(phenylthio)butan-2-ylamino)phenylsulfonyl)benzamide 
• 852808-20-9 N-(4-(4-((4′-chloro(1,1′-biphenyl)-2-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(dimethylamino)-1-((phenylsulfanyl)methyl)propyl)amino)-3-(trifluoromethyl)benzenesulfonamide 
• 852809-60-0 (R)-4-(-4-((4'-chlorobiphenyl-2-yl)methyl)piperazin-1-yl)-N-(4-(4-(dimethylamino)-1-(phenylthio)butan-2-ylamino)phenylsulfonyl)benzamide 
• 1065604-19-4 N-(4-bromo-3-methylphenylsulfonyl)-4-(4-((4'-chlorophenyl-2-yl)methyl)piperazin-1-yl)benzamide 
• 1382034-49-2 C₃₄H₃₈ClN₃O₃S 
• 1382034-53-8 C₃₅H₄₀ClN₃O₃S 
• 1382034-45-8 C₂₄H₂₂Cl₂N₂O 
• 1382034-47-0 C₂₆H₂₈ClN₃O₃S 
• 1382034-48-1 C₂₈H₃₂ClN₃O₃S 

Relevant academic research and scientific papers

INHIBITING B-CELL LYMPHOMA 2 (BCL-2) AND RELATED PROTEINS

Novel compounds inhibiting anti-apoptosis proteins B-cell lymphoma 2 (Bcl-2) and Bcl-XL include compounds of formula (I) and formula (II) disclosed herein, as well as liposome compositions comprising Bcl-2 inhibitor compounds. These compositions are usefu

ACYLSULFONAMIDE DERIVATIVES FOR TREATING SENESCENCE-ASSOCIATED DISEASES AND DISORDERS

Compounds represented by Formula (I) and (II) and salts thereof are described herein. The compounds or salts of Formula (I) and (II) may be used to treat senescence-associated diseases and disorders.

APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES

Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.

APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES

Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.

BCL-2 INHIBITORS CONTAINING A ZINC BINDING MOIETY

The present invention relates to Bcl-2 inhibitors and their use in the treatment of cell proliferative diseases such as cancer. The compounds of the invention may further act as HDAC inhibitors

Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL

Overexpression of the antiapototic proteins Bcl-2 and Bcl-xL provides a common mechanism through which cancer cells gain a survival advantage and become resistant to conventional chemotherapy. Inhibition of these prosurvival proteins is an attractive strategy for cancer therapy. We recently described the discovery of a selective Bcl-xL antagonist that potentiates the antitumor activity of chemotherapy and radiation. Here we describe the use of structure-guided design to exploit a deep hydrophobic binding pocket on the surface of these proteins to develop the first dual, subnanomolar inhibitors of Bcl-xL and Bcl-2. This study culminated in the identification of 2, which exhibited EC50 values of 8 nM and 30 nM in Bcl-2 and Bcl-xL dependent cells, respectively. Compound 2 demonstrated single agent efficacy against human follicular lymphoma cell lines that overexpress Bcl-2, and efficacy in a murine xenograft model of lymphoma when given both as a single agent and in combination with etoposide.