31847-22-0

Upstream product

• 97-52-9 2-methoxy-4-nitrophenylamine 
• 31863-04-4 N-(2-methoxy-4-nitro-benzen)-ethylcarbamate 

Downstream Products

• 308125-06-6 N-(2-methoxy-4-methanesulfonamido-benzen)-ethylcarbamate 
• 1005030-61-4 ethyl N-(4-amino-5-iodo-2-methoxybenzene)carbamate 
• 57165-06-7 N-(4-amino-3-methoxyphenyl)methanesulfonamide 

Relevant academic research and scientific papers

SUBSTITUTED P-DIAMINOBENZENE DERIVATIVES

The present invention relates to aniline derivatives of the general formula I or pharmaceutically acceptable salts thereof and their use.

Synthesis and antiproliferative activity of some variously substituted acridine and azacridine derivatives

A group of 9-substituted acridine and azacridine derivatives (m-AMSA analogues) were synthesised following classical procedures as potential antitumour agents with inhibitory effects on DNA topoisomerase II. Some were found to have noticeable cytotoxicity against human HL-60 and HeLa cells grown in culture. Their non-covalent interactions with calf thymus DNA have been studied using fluorescence quenching. We evaluated DNA damage produced by the tested compounds by means of DNA filter elution and protein precipitation techniques. Catalytic studies carried out with purified topoisomerase confirmed these agents as antitopoisomerase inhibitors. Chemotherapy of solid-tumour-bearing mice with tested compounds allowed an aza-analogue (compound IIIb), as potent as m-AMSA but less toxic towards the host, to be recognised. (C) 2000 Editions scientifiques et medicales Elsevier SAS.

Pyrrolo-quinoline derivatives as potential antineoplastic drugs

Some novel pyrrolo-quinoline derivatives have been synthesized as potential antineoplastic agents. They contain an angular aromatic tricyclic or tetracyclic system, to which the methanesulfon-anisidide side chain typical of amsacrine as such, or lacking the m-methoxy substituent, is connected. A methyl group can be present at position 7 of the pyrrolo-quinoline ring. The novel compounds exhibit interesting cell growth inhibitory properties when tested against the NCI panel of cell lines, in particular those obtained from solid tumors like CNS-, melanoma- and prostate-derived cells. The mechanism of cytotoxic action does not seem to be related to topoisomerase II poisoning ability. Most active proved to be compound 4a, which lacks both methyl and methoxy substituents, followed by 5a, having the methoxy group only. Biological activity is less pronounced in the tetracyclic family of derivatives 6 and 7. Copyright (C) 2000 Elsevier Science Ltd.