Hydrazide pharmaceuticals as conjugates to polyaldehyde dextran: syntheses, characterization, and stability.
The coupling of ellipticine and CI-921, two antineoplastic pharmaceuticals, to polyaldehyde dextran can be carried out under mild reaction conditions with novel acid hydrazides of the parent drugs. The resulting acyl hydrazones resist hydrolytic and enzymatic cleavage and offer a method for drug loading via dextran conjugates to monoclonal antibodies.
Heindel
N D
ND
Institute for Health Sciences and Department of Chemistry, Lehigh University, Bethlehem, Pennsylvania 18015.
Zhao
H R
HR
Leiby
J
J
VanDongen
J M
JM
Lacey
C J
CJ
Lima
D A
DA
Shabsoug
B
B
Buzby
J H
JH
D000677:Amsacrine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry; D000818:Animals; D000970:Antineoplastic Agents; D003911:Dextrans / Q000138:chemical synthesis* / Q000737:chemistry; D004355:Drug Stability; D004611:Ellipticines / Q000138:chemical synthesis* / Q000737:chemistry; D004798:Enzymes / Q000097:blood; D006835:Hydrazones / Q000138:chemical synthesis* / Q000737:chemistry; D006868:Hydrolysis; D007202:Indicators and Reagents; D051381:Rats
D000970:Antineoplastic Agents; C069067:CI 921-polyaldehyde dextran; D003911:Dextrans; D004611:Ellipticines; D004798:Enzymes; D006835:Hydrazones; D007202:Indicators and Reagents; C069065:ellipticine-polyaldehyde dextran; D000677:Amsacrine; C034192:ellipticine; C042315:asulacrine