[Alkylating derivatives of 2-amino-2-deoxysugars and 1-methylamino-1-deoxypolyols (synthesis and experimental study)].
A number of derivatives of 2-amino-2-deoxysaccharides and 1-methylamino-1-deoxypolyols acylated by cytotoxic phenylalkanic and amino acids were synthesized and experimentally tested for antitumor activity. Some compounds showed a high antitumor activity against plasmacytoma MOPC-406: a 2-fold increase in experimental animals survival and a 80--100% cure rate were observed. Physicochemical properties, particularly, stability in aqueous solution and antitumor activity of one of the most potent compounds--1-methylamino-1-deoxy-1-N[p-di(2-chloroethyl) aminophenylacetyl]-D-glucitol (Agluphen)--are described in detail.
Shkodinskaia
E N
EN
Dorn
H
H
Vasina
O S
OS
Kashnikova
N M
NM
Kikot'
B S
BS
D000477:Alkylating Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000605:Amino Alcohols / Q000138:chemical synthesis* / Q000494:pharmacology; D000606:Amino Sugars / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis*; D003837:Deoxy Sugars / Q000138:chemical synthesis* / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D051379:Mice; D009374:Neoplasms, Experimental / Q000188:drug therapy; D013329:Structure-Activity Relationship
D000477:Alkylating Agents; D000605:Amino Alcohols; D000606:Amino Sugars; D000970:Antineoplastic Agents; D003837:Deoxy Sugars
Alkiliruiushchie proizvodnye 2-amino-2-dezoksisakharov i 1-metilamino-1-dezoksipoliolov (sintez i éksperimental'noe izuchenie).