265645-64-5

Upstream product

• 62978-52-3 melphalan methyl ester hydrochloride salt 
• 121031-01-4 5-bromo-β,β,2,4-tetramethyl-3,6-dioxo-1,4-cyclohexadiene-1-propanoic acid 
• 409316-82-1 2-bromo-3,5-dimethyl-hydroquinone 
• 409316-81-0 2-bromo-3,5-dimethylcyclohexane-2,5-diene-1,4-dione 
• 148-82-3 L-PAM 
• 541-47-9 3-Methylbutenoic acid 

Downstream Products

• 88457-23-2 (S)-2-amino-3-(4-bis(2-chloroethyl)aminophenyl)propionoic acid methyl ester 
• 121031-01-4 5-bromo-β,β,2,4-tetramethyl-3,6-dioxo-1,4-cyclohexadiene-1-propanoic acid 

Relevant academic research and scientific papers

Reductive and Bioreductive Activation is Controlled by Electronic Properties of Substituents in Conformationally-Constrained Anticancer Drug Delivery Systems

Conformationally-constrained, anticancer drug delivery systems (TDDS) containing the methyl ester of melphalan (as a model drug) were synthesized using electron-withdrawing or electron-donating functional groups to modulate reductive and bioreductive activation. The electronic nature of substituents in TDDS was found to control reductive and bioreductive activation of TDDS, thus influencing drug delivery from TDDS.

Reductive activation of conformationally-constrained, anticancer drug delivery systems

Redox-active substituents were used to modulate reduction potentials in conformationally-constrained, drug delivery systems. The extent of drug delivery was proportional to the degree of reductive activation, which was influenced by the electronic properties of the substituents. Such reductively-activated carrier systems can be used to achieve controlled drug delivery to bioreductive regions in hypoxic solid tumors.