Synthesis and biological evaluation of a water soluble phosphate prodrug of 3-aminopyridine-2-carboxaldehyde thiosemicarbazone (3-AP).
With the aim of improving its biological and pharmaceutical profiles, two water soluble phosphate prodrugs of 3-AP, 3a and 3b were prepared. The detailed synthesis and the preliminary evaluation of these prodrugs are described.
Li
J
J
Vion Pharmaceutical, Inc., Four Science Park, New Haven, CT 06511, USA.
Luo
X
X
Wang
Q
Q
Zheng
L M
LM
King
I
I
Doyle
T W
TW
Chen
S H
SH
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004285:Dogs; D004355:Drug Stability; D051379:Mice; D008807:Mice, Inbred BALB C; D011355:Prodrugs / Q000138:chemical synthesis* / Q000494:pharmacology; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D012995:Solubility; D013882:Thiosemicarbazones / Q000138:chemical synthesis* / Q000494:pharmacology
D000970:Antineoplastic Agents; D011355:Prodrugs; D011725:Pyridines; D013882:Thiosemicarbazones; C078157:3-aminopyridine-2-carboxaldehyde thiosemicarbazone