NEW MATERIAL:Tf-NCS [Melting point; 230°C (decomposition); Elementary analysis; C, 44W50%; H, 6W7%; N, 13W16%; S, 0.3W0.8%; Molecular weight; 90,000W130,000 (measured by the gel filtration method); Solubility; Soluble in water and insoluble in methanol, etc. Color reaction; Positive to Rydon-Smith reagent, biuret reaction, etc.].
USE: A selective carcinostatic agent.
PREPARATION: Transferrin Tf-NH2 is reacted with SPDP expressed by formula I to give a compound expressed by formula II. Neocarzinostatin NCS-NH2 is then reacted with the SPDP expressed by formula I to afford a compound expressed by formula III, which is reacted with a compound expressed by formula IV to give a compound expressed by formula V. The above-mentioned compound expressed by formula II is reacted with the compound expressed by formula V to afford the aimed Tf-NCS expressed by formula VI which is an excellent carcinostatic agent surrounded by cancer cells having Tf receptors to cause DNA damage and exhibit cellulicidal effect of 2W10 times based on the NCS.
KOUGO YUTAKA
KONDO HITOSHI
NISHISATO TAKUJI
NIITSU YOJIRO
KOIDE YOSHIO
ITO AKIRA
ICHIKAWA KIYOHIDE
URUSHIZAKI ICHIRO
KOUGO YUTAKA
| JPS59199635A | 1984-11-12 |