fosbretabulin and Lymphoma--Large-B-Cell--Diffuse

fosbretabulin has been researched along with Lymphoma--Large-B-Cell--Diffuse* in 1 studies

Other Studies

1 other study(ies) available for fosbretabulin and Lymphoma--Large-B-Cell--Diffuse

Article	Year
Potent, orally active heterocycle-based combretastatin A-4 analogues: synthesis, structure-activity relationship, pharmacokinetics, and in vivo antitumor activity evaluation. Journal of medicinal chemistry, 2002, Apr-11, Volume: 45, Issue:8 The synthesis and structure-activity relationship study of a series of compounds with heterocycles in place of the cis double bond in combretastatin A-4 (CA-4) are described. Substituted tosylmethyl isocyanides were found to be the key intermediates in construction of the heterocycles. Cytotoxicities of the heterocycle-based CA-4 analogues were evaluated against NCI-H460 and HCT-15 cancer cell lines. 3-Amino-4-methoxyphenyl and N-methyl-indol-5-yl were the best replacements for the 3-hydroxy-4-methoxyphenyl in CA-4. 4,5-Disubstituted imidazole was found to be the best for the replacement of the cis double bond in CA-4. Medicinal chemistry efforts led to the discovery of compounds 24h and 25f that were found to be 32 and 82% bioavailable, respectively, in rat. Evaluation of 24h and 25f against murine M5076 reticulum sarcoma in mice revealed that both compounds were orally efficacious with an increase in life span of 38.5 and 40.5%, respectively. Topics: Administration, Oral; Animals; Antineoplastic Agents; Biopolymers; Cell Division; Dogs; Drug Screening Assays, Antitumor; Haplorhini; Humans; Imidazoles; Lymphoma, Large B-Cell, Diffuse; Mice; Mice, Nude; Neoplasm Transplantation; Rats; Stilbenes; Structure-Activity Relationship; Transplantation, Heterologous; Tubulin; Tumor Cells, Cultured	2002

Article

Year

Potent, orally active heterocycle-based combretastatin A-4 analogues: synthesis, structure-activity relationship, pharmacokinetics, and in vivo antitumor activity evaluation.

Journal of medicinal chemistry, 2002, Apr-11, Volume: 45, Issue:8

The synthesis and structure-activity relationship study of a series of compounds with heterocycles in place of the cis double bond in combretastatin A-4 (CA-4) are described. Substituted tosylmethyl isocyanides were found to be the key intermediates in construction of the heterocycles. Cytotoxicities of the heterocycle-based CA-4 analogues were evaluated against NCI-H460 and HCT-15 cancer cell lines. 3-Amino-4-methoxyphenyl and N-methyl-indol-5-yl were the best replacements for the 3-hydroxy-4-methoxyphenyl in CA-4. 4,5-Disubstituted imidazole was found to be the best for the replacement of the cis double bond in CA-4. Medicinal chemistry efforts led to the discovery of compounds 24h and 25f that were found to be 32 and 82% bioavailable, respectively, in rat. Evaluation of 24h and 25f against murine M5076 reticulum sarcoma in mice revealed that both compounds were orally efficacious with an increase in life span of 38.5 and 40.5%, respectively.

Topics: Administration, Oral; Animals; Antineoplastic Agents; Biopolymers; Cell Division; Dogs; Drug Screening Assays, Antitumor; Haplorhini; Humans; Imidazoles; Lymphoma, Large B-Cell, Diffuse; Mice; Mice, Nude; Neoplasm Transplantation; Rats; Stilbenes; Structure-Activity Relationship; Transplantation, Heterologous; Tubulin; Tumor Cells, Cultured

2002