61588-93-0

Usage

Chemical family

Spirocyclic lactam

Target protein

BRD4 (bromodomain-containing protein 4)

Function

Potent and selective inhibitor of BRD4

Role of target protein

Regulation of gene expression and cell proliferation

Potential therapeutic applications

Cancer treatment (leukemia, lymphoma, solid tumors), inflammatory and autoimmune diseases

Mechanism of action

Inhibits the growth and survival of cancer cells, modulates the immune response

Current status

Being studied in preclinical and early-phase clinical trials

Upstream product

• 67950-95-2 1-carboxycyclohexylacetic acid 
• 100-63-0 phenylhydrazine 

Relevant academic research and scientific papers

Synthesis, physicochemical and anticonvulsant properties of N-benzyl and N-aminophenyl derivatives of 2-azaspiro[4.4]nonane and [4.5]decane-1,3-dione. Part I

To continue our systematic SAR studies, two series of N-benzyl- (X = CH2) and N-aminophenyl- (X = NH) derivatives of 2-azaspiro[4.4]nonane (1a-1j) and 2-azaspiro[4.5]decane-1,3-dione (2a-2j) were synthesized, and evaluated in maximum electroshock seizure (MES), subcutaneous pentylenetetrazole (sc.MET) and rotorod (TOX) tests for their anticonvulsant activity. Among those derivatives, the most potent N-aminophenyl-2-azaspiro[4.4]nonane-1,3-dione 1j had ED50 = 76.27 mg kg-1. X-ray structures for two pairs of derivatives with a different linker were solved. Then 3-D data for the active 1j versus less active 2j, both having an imine linker (X = NH), and the respective parent of compounds with a methylene linker (X = CH2) (1a and 2a) were discussed.