Dimethanesulphonate esters in receptor mapping studies. 1. Benzene 1,2-, 1,3- and 1,4-diol, dimethanol and diethanol dimethanesulphonates and anti-tumour activity

Autor:	B W, Fox, J A, Hadfield, P M, O'Connor
Rok vydání:	1991
Předmět:	Male Models Molecular Binding Sites Receptors Drug Body Weight Antineoplastic Agents Methyl Methanesulfonate Rats Lethal Dose 50 Structure-Activity Relationship Isomerism Solubility Tumor Cells Cultured Animals Computer Simulation Half-Life
Zdroj:	Anti-cancer drug design. 6(2)
ISSN:	0266-9536
Popis:	The anti-tumour activities of nine aromatic dimethanesulphonate esters were examined. Their biological effects have been related to both their chemical reactivity and to the computer-modelled vectorial positions of the centres of alkylation of the compounds. One compound (19) has shown activity between sensitive and resistant Yoshida tumours in vivo and also shows the highest activity between these two cell lines in vitro. In its minimal energy form, this compound would require to interact with converging nucleophilic centres about 6 A apart, and it is tentatively suggested that this may be an appropriate dimension for a receptor which is required to be alkylated in order to show anti-tumour activity.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=pmid________::a6ab12f2b2fca15efd2ca5d4cb1cf5bb https://pubmed.ncbi.nlm.nih.gov/2039583 Zobrazit plný text záznamu