CAS: 106401-68-7; 14-Bromo-13-Dimethylketal-Daunorubicin

主要参考文献

参考标题:Synthesis And Antitumor Activity Of New D-Galactose-Containing Derivatives Of Doxorubicin
作者:Eugenia N. Olsufyeva,Anna N. Tevyashova,Ivan D. Trestchalin,Maria N. Preobrazhenskaya,David Platt,Anatole Klyosov |发布日期:2003.6
摘要:A General Scheme Of Synthesis Of Antibiotic Doxorubicin Derivatives Is Based On The 13-Dimethyl Ketal Of 14-Bromodaunorubicin (4). The Interaction Of 4 With Melibiose (5), Lactose (6), 3-Methoxy-4-O-(2,3,4,6-Tetra-O-Acetyl-Beta-D-Galactopyranosyl)-4-Oxybenzaldehyde (12) Or 4-O-(2,3,4,6-Tetra-O-Acetyl-Beta-D-Galactopyranosyl)-4-Oxybenzaldehyde (13) By Reductive Alkylation Followed By Hydrolysis Of The Corresponding Intermediate Bromoketals Produced 3'-N-[alpha-D-Galactopyranosyl-(1-->6)-O-1-Deoxy-D-Glucit-1-Yl]Doxorubicin (7), 3'-N-[beta-D-Galactopyranosyl-(1-->4)-O-1-Deoxy-D-Glucit-1-Yl]Doxorubicin (8), 3'-N-[3"-Methoxy-4"-O-(Beta-D-Galactopyranosyl)-4"-Oxybenzyl]Doxorubicin (16), And 3'-N-[4"-O-(Beta-D-Galactopyranosyl)-4"-Oxybenzyl]Doxorubicin (17). Cytotoxic And Antitumor Activity Of The Synthesized Drug Candidates Compared To The Parent Doxorubicin Was Studied Using Various Experimental Models, In Particular, On Mice Bearing Lymphocyte Leukemia P-388 At Single And Multiple I.V. Injection Regimens. (C) 2003 Elsevier Science Ltd. All Rights Reserved.