u-71184 has been researched along with adozelesin* in 2 studies
2 other study(ies) available for u-71184 and adozelesin
| Article | Year |
|---|---|
Synthesis, cytotoxicity, antitumor activity and sequence selective binding of two pyrazole analogs structurally related to the antitumor agents U-71,184 and adozelesin.
Two pyrazole analogs structurally related to the antitumor agents adozelesin and U-71,184 respectively were synthesized. By using a polymerase chain reaction approach, both compounds show selective binding to A + T rich sequences exactly as reference compound U-71,184. In in vitro assays, against L1210 cell lines, both derivatives showed cytotoxicity in the pM range, values comparable with the natural target compound (+)-CC-1065. The most active compound showed very high antitumor activity in mice implanted with L1210 cells (ILS% 363). Topics: Animals; Antineoplastic Agents; Benzofurans; Binding Sites; Cyclohexanecarboxylic Acids; Cyclohexenes; Duocarmycins; Indoles; Leukemia L1210; Magnetic Resonance Spectroscopy; Mice; Neoplasm Transplantation; Polymerase Chain Reaction; Pyrazoles; Spectrophotometry, Infrared | 1997 |
Total synthesis and biological properties of novel antineoplastic (chloromethyl)furanoindolines: an asymmetric hydroboration mediated synthesis of the alkylation subunits.
1,2-Dihydro-1-(chloromethyl)-5-hydroxy-8-methyl-3H-furano[3,2-e]in dole (CFI) as a novel replacement of the cyclopropylpyrroloindoline (CPI) alkylation subunit of CC-1065, U-71184, and U-73975 (adozelesin) has been synthesized and incorporated into a series of efficacious antineoplastic agents. A partial solution to an asymmetric synthesis of the CFI alkylation subunit has been achieved by the implementation of an asymmetric hydroboration reaction of an intermediate 3-methyleneindoline (13). Extension to the asymmetric synthesis of the CBI and CI alkylation subunits is presented. The demonstration and comparative study of the sequence-selective DNA alkylation properties of the CFI-based agents are detailed, and the preliminary in vitro and in vivo antineoplastic properties of these agents in the human epidermoid cell lung carcinoma (T222) are described. Topics: Alkylation; Animals; Antineoplastic Agents; Base Sequence; Benzofurans; Boron Compounds; Carcinoma, Squamous Cell; Cyclohexanecarboxylic Acids; Cyclohexenes; DNA; Drug Screening Assays, Antitumor; Duocarmycins; Female; Furans; Humans; Indoles; Leucomycins; Lung Neoplasms; Mice; Mice, Nude; Molecular Sequence Data; Tumor Cells, Cultured | 1994 |