Antitumor activity of the novel melphalan containing tripeptide J3 (L-prolyl-L-melphalanyl-p-L-fluorophenylalanine ethyl ester): comparison with its m-L-sarcolysin analogue P2.

The novel melphalan prodrug J1 inhibits neuroblastoma growth in vitro and in vivo.

Neuroblastoma is the most common extracranial solid tumor of childhood. The activity of J1 (l-melphalanyl-p-l-fluorophenylalanine ethyl ester), an enzymatically activated melphalan prodrug, was evaluated in neuroblastoma models in vitro and in vivo. Seven neuroblastoma cell lines with various levels of drug resistance were screened for cytotoxicity of J1 alone or in combination with standard cy...

Selective tumor apoptosis by MF13, L-prolyl-L-m-[bis(chloroethyl)amino]-phenylalanyl-L-norvaline ethyl ester, a new sarcolysin containing tripeptide.

ID50 and ID90 values for L-prolyl-L-m-[bis(chloroethyl)amino]-phenylalanyl-L-norvaline ethyl ester HCl (MF13), were determined in four murine (leukemia, lymphoma, melanoma, and lung) and eight human cancer cell lines (two leukemia, prostate, kidney, colon, two melanoma, and breast). Cytotoxic activity was 2-5 times higher than that of sarcolysin [(L-3-[bis(2-chloroethyl)amino]-L-phenylalanine] ...

The effects of DL-p-fluorophenylalanine and L-3-nitrotyrosine on the growth and biochemistry of the Taper liver tumor.

Two amino acid analogs, DL-p-fluorophenylalanine and L-3-nitrotyrosine, retarded the growth of Taper liver tumor in mice and increased mouse survival time. Both of the analogs were taken into the tumor cells in vitro and in vivo, and DL-p-fluorophenylalanine inhibited the uptake of L-phenylalanine in vitro. tRNA in the "pH 5 fraction" from tumor cells could be acylated with DL-p-fluorophenylala...

Diet and Cholesterolemia. Vii. Effects of Methionine, Ethionine, and P-fluorophenylalanine.

The Effects of DL-/?-FluorophenylaIanine and L-3-Nitrotyrosine on the Growth and Biochemistry of the Taper Liver Tumor1

Two amino acid analogs, DL-p-fluorophenylalanine and L-3-nitrotyrosine, retarded the growth of Taper liver tumor in mice and increased mouse survival time. Both of the analogs were taken into the tumor cells in vitro and in vivo, and DL-p-fluorophenylalanine inhibited the uptake of L-phenylalanine in vitro. tRNA in the "pH 5 fraction" from tumor cells could be acylated with DL-p-fluorophenylala...