title: Synthesis and antitumor activity of 3- and 5-hydroxy-4-methylpyridine-2-carboxaldehyde thiosemicarbazones.
abstract: 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.
authors.affiliation: Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut 06510.
authors.forename: Y
authors.initials: Y
authors.lastname: Wang
authors.forename: M C
authors.initials: MC
authors.lastname: Liu
authors.forename: T S
authors.initials: TS
authors.lastname: Lin
authors.forename: A C
authors.initials: AC
authors.lastname: Sartorelli
mesh_terms: 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
chemical_list: D000970:Antineoplastic Agents; D011725:Pyridines; D013882:Thiosemicarbazones; C078156:5-hydroxy-4-methylpyridine-2-carboxaldehyde thiosemicarbazone; C078155:3-hydroxy-4-methylpyridine-2-carboxaldehyde thiosemicarbazone