348642-85-3

Upstream product

• 2973-80-0 2-bromo-5-hydroxybenzaldehyde 
• 677-22-5 tert-butylmagnesium chloride 
• 100-83-4 meta-hydroxybenzaldehyde 

Downstream Products

• 348642-87-5 3-[4-benzyloxy-2-(1,2-dimethyl-propenyl)-phenyl]-2-(tert-butyl-dimethyl-silanyloxymethyl)-5-oxo-pyrrolidine-1-carboxylic acid tert-butyl ester 
• 348642-88-6 6-benzyloxy-3-(tert-butyl-dimethyl-silanyloxymethyl)-8-isopropyl-8-methyl-1-oxo-3,3a,8,8a-tetrahydro-1H-2-aza-cyclopenta[a]indene-2-carboxylic acid tert-butyl ester 
• 348642-89-7 6-benzyloxy-3-(tert-butyl-dimethyl-silanyloxymethyl)-8-isopropyl-8-methyl-1-oxo-3,3a,8,8a-tetrahydro-1H-2-aza-cyclopenta[a]indene-2-carboxylic acid tert-butyl ester 
• 348642-86-4 4-Benzyloxy-1-bromo-2-(1,2-dimethyl-propenyl)-benzene 

Relevant academic research and scientific papers

Rational design, synthesis, and biological evaluation of rigid pyrrolidone analogues as potential inhibitors of prostate cancer cell growth

In view of its role in tumor promotion and signal transduction, protein kinase C (PKC) has proven to be an exciting target for cancer therapy. With the aid of molecular modeling, we rationally designed and stereoselectively synthesized a new class of rigidified pyrrolidone-based PKC activators. Pyrrolidone 15 was found to exhibit reasonable affinity for PKCδ, with lower affinity for the other isozymes tested. Pyrrolidone 2 causes the dose-dependent induction of apoptosis in LNCaP prostate cancer cells. This apoptotic effect could be markedly potentiated by the use of LNCaP cells overexpressing the PKCα or δ isozymes.

Rigid pyrrolidone modulators of pkc

Compounds of the general formula (I): wherein substituents at R1, R2, R3 and R4 have any of the values defined in the specification, and their pharmaceutically acceptable salts, are PKC modulators and are useful for treating diseases, such as, for example, cancers including prostate cancer, inflammatory, autoimmune and neurological disorders including Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising compounds of formula (I), processes for preparing compounds of formula (I), and intermediates useful for preparing compounds of formula (I).