185424-66-2

Upstream product

• 128781-07-7 5,6,7-trimethoxy-1H-indole-2-carboxylic acid 
• 157160-99-1 4-Chloro-3-nitrobenzoic acid tert-butyl ester 
• 96-99-1 4-chloro-3-nitrobenzoate 
• 38818-50-7 4-chloro-3-nitro-benzoyl chloride 
• 185424-65-1 6-[(benzyloxycarbonyl)amino]-1-(t-butyloxycarbonyl)-3-[(methanesulfonyloxy)methyl]indoline 
• 185424-59-3 dimethyl [4-(benzyloxycarbonyl)-amino-2-nitrophenyl]malonate 
• 185424-64-0 6-[(benzyloxycarbonyl)amino]-1-(t-butyloxycarbonyl)-3-(hydroxymethyl)indoline 
• 185424-63-9 2-[4-(benzyloxycarbonyl)amino-2-(t-butyloxycarbonyl)aminophenyl]propane-1,3-diol 
• 185424-60-6 2-[4-(benzyloxycarbonyl)amino-2-nitrophenyl]propane-1,3-diol 
• 185424-58-2 Dimethyl (4-carboxy-2-nitrophenyl)malonate 
• 185424-61-7 2-[2-amino-4-(benzyloxycarbonyl)aminophenyl]propane-1,3-diol 

Relevant academic research and scientific papers

Radiation-activated cytotoxin therapy of neoplastic disease

A method of treating neoplastic disease wherein a patient in need of such treatment is administered an effective amount of a radiation-activated cytotoxin prodrug (RACP) which has low toxicity, which is reducible by reducing agents generated by the radiol

Cyclopropylindoles and their seco precursors, and their use as prodrugs

The present invention provides compounds of formula (I) and (II) which may be used as anticancer drugs.

Synthesis of nitrogen and sulfur analogues of the seco-CI alkylating agent

Two complementary syntheses of amino seco-CI (CI = 1a,2,3,5-tetrahydro-1H-cycloprop[1,2-c]indol-5-one) alkylating agents starting from isomeric chloronitrobenzoic acids are reported. Further reactions of these compounds, including diazotisation to phenol and thiophenol derivatives, and alkylation and acylation reactions relevant to the preparation of pro-drug forms are also described.

Nitrogen and sulfur analogues of the seco-CI alkylating agent: Synthesis and cytotoxicity

The first synthesis of seco-CI alkylating agents bearing a nitrogen or sulfur substituent in place of the oxygen at C-6 is described. In comparison with a phenol, an amino substituent confers reduced but significant cytotoxicity, even when mono- or dimethylated, while sulfur analogues are considerably less potent.