Synthesis and antitumor activity of 3- and 5-hydroxy-4-methylpyridine-2-carboxaldehyde thiosemicarbazones.
To develop an alpha-(N)-heterocyclic carboxaldehyde thiosemicarbazone with clinical utility as an anticancer agent, two analogues, 3-hydroxy-4-methylpyridine-2-carboxaldehyde thiosemicarbazone (3-HMP) and 5-hydroxy-4-methylpyridine-2-carboxaldehyde thiosemicarbazone (5-HMP), of 5-hydroxypyridine-2-carboxaldehyde thiosemicarbazone (5-HP) have been designed and synthesized by two different methods. 3-HMP and 5-HMP both showed better antitumor activity than their respective parent compounds, 3-hydroxypyridine-2-carboxaldehyde thiosemicarbazone and 5-HP, in mice bearing the L1210 leukemia.
Wang
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Y
Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut 06510.
Liu
M C
MC
Lin
T S
TS
Sartorelli
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AC
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis*; D005260:Female; D007939:Leukemia L1210 / Q000188:drug therapy; D051379:Mice; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D013882:Thiosemicarbazones / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use
D000970:Antineoplastic Agents; D011725:Pyridines; D013882:Thiosemicarbazones; C078156:5-hydroxy-4-methylpyridine-2-carboxaldehyde thiosemicarbazone; C078155:3-hydroxy-4-methylpyridine-2-carboxaldehyde thiosemicarbazone