title: Enhancement of anti-proliferative activities of 5-FU, HCFU, SN-38, THP and ACNU by a serine protease inhibitor, FOY-305.
abstract: The effects of a synthetic serine protease inhibitor, FOY-305, on the proliferation of normal and transformed mouse fibroblasts were investigated in vitro by MTT colorimetric assay. FOY-305 inhibited the growth of normal NIH3T3 cells and their src- and erbB2-transformed cells with a half maximum inhibitory concentration (IC50) of 1-1.2 mg/ml whereas it suppressed the growth of ras-transformed cells more effectively (IC50 was 0.5-0.6 mg/ml). Flow cytometric analysis using synchronized NIH3T3 cells has shown that the growth-inhibitory activity of FOY-305 was due to the suppression of G(1)/S transition. The synergistic effects between FOY-305 and traditional anticancer drugs were also investigated by the MTT assay and the results showed that FOY-305 significantly enhanced the antiproliferative activities of 5-fluorouracil (5-FU), 1-hexylcarbamoyl-5-fluorouracil (HCFU), 7-ethyl-1-hydroxy-7-ethyl-10-[4-(1-piperidino)-1-piperidino] camptothecin (SN-38), pirarubicin (THP) and 1-(4-amino-2-methyl-5-pyrimidinyl)-methyl-(2-chloroethyl)-3-nitrosourea hydrochloride (ACNU).
authors.affiliation: CHIBA CANC CTR,RES INST,DIV ANIM RES,CHUO KU,CHIBA 260,JAPAN. CHIBA CANC CTR,RES INST,CLIN LAB,CHUO KU,CHIBA 260,JAPAN. MITSUI PHARMACEUT INC,POSTMKT SURVEILLANCE DEPT,CHUO KU,TOKYO 103,JAPAN. UNIV TOKYO,FAC MED,DEPT ORAL SURG,BUNKYO KU,TOKYO 113,JAPAN.
authors.forename: T
authors.initials: T
authors.lastname: Hiwasa
authors.forename: H
authors.initials: H
authors.lastname: Tokita
authors.forename: M
authors.initials: M
authors.lastname: Hirose
authors.forename: Y
authors.initials: Y
authors.lastname: Ike
authors.forename: M
authors.initials: M
authors.lastname: Ohkoshi