680199-06-8

Upstream product

• 944088-78-2 2-[N-(2-bromoethyl)-2,4-dinitro-6-({[2-(tetrahydro-2H-pyran-2-yloxy)ethyl]amino}carbonyl)anilino]ethyl methanesulfonate 
• 1221752-39-1 2-(bis(2-chloroethyl)amino)-3,5-dinitrobenzoic acid 
• 851627-22-0 2-(bis(2-bromoethyl)amino)-N-(2-hydroxyethyl)-3,5-dinitrobenzamide 
• 2386-52-9 silver methanesulfonate 
• 2213-79-8 methyl 2-chloro-3,5-dinitrobenzoate 
• 1221752-41-5 2-[bis(2-chloroethyl)amino]-3,5-dinitrobenzoyl chloride 
• 2497-91-8 2-chloro-3,5-dinitrobenzoic acid 
• 680199-55-7 2-[{2-[(methylsulfonyl)oxy]ethyl}-4,6-dinitro-6-({[2-(tetrahydro-2H-pyran-2-yloxy)ethyl] amino}carbonyl)anilino] ethyl methanesulfonate 

Downstream Products

• 1012063-54-5 (4S,5S)-6-[2-[2-[(2-bromoethyl)[2-(methylsulfonyloxy)ethyl]amino]-3,5-dinitrobenzamido]-ethoxy]-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid 
• 950998-58-0 C₂₂H₃₅⁽³⁾HBrN₄O₁₂PS 
• 950998-57-9 C₁₄H₁₈⁽³⁾HBrN₄O₉S 
• 950998-56-8 2-((2-bromoethyl)-2,4-dinitro-6-(((2-oxoethyl)amino)carbonyl)anilino)ethyl methanesulfonate 

Relevant academic research and scientific papers

Synthesis and evaluation of new dinitrobenzamide mustards in human prostate cancer

Tumor hypoxia has been widely explored over the years as a diagnostic and therapeutic marker. Herein, we have reported the design and synthesis of a series of dinitrobenzamide mustards (DNBM) based on the PR-104A hypoxia-selective prodrug. Specifically, we explored the impact of various leaving groups and the introduction of a carboxylic acid group on the biological performance of the DNBM constructs. Once in hand, the Log D values, cytotoxicity in PC-3 and DU-145 human prostate cancer cells lines and the hypoxia selectivities of the DNBM analogs were examined. Overall, the DNBM constructs were found to be tolerant to modifications with none of the explored modifications substantially degrading the cytotoxic potential of the constructs.

PROCESSES OF PREPARING ASYMMETRIC DINITROBENZAMIDE MUSTARD COMPOUNDS, INTERMEDIATE COMPOUNDS USEFUL THEREIN AND PRODUCTS OBTAINED THEREFROM

The invention relates to methods of preparing compounds of formula (II) wherein Z represents -OR1 or -N(R2)R2a-, where R1 is lower alkylene (C1-C6), R2 is lower alkyl or H and R

NOVEL NITROPHENYL MUSTARD AND NITROPHENYLAZIRIDINE ALCOHOLS AND THEIR CORRESPONDING PHOSPHATES AND THEIR USE AS TARGETED CYTOTOXIC AGENTS

The present invention relates to novel nitrophenyl mustard and nitrophenylaziridine alcohols, to their corresponding phosphates, to their use as targeted cytotoxic agents; as bioreductive drugs in hypoxic tumours, and to their use in cell ablation, includ

NITROANILINE-BASED ALKYLATING AGENTS AND THEIR USE AS PRODRUGS

Nitroaniline-based unsymmetrical mustards of the general formula (I) are provided, together with methods of preparation and methods for their use as produgs for gene-dependent enzyme prodrug therapy (GDEPT) and cell ablation therapy in conjuction with nit