cryptophycin-52 and Pancreatic-Neoplasms

cryptophycin-52 has been researched along with Pancreatic-Neoplasms* in 2 studies

Other Studies

2 other study(ies) available for cryptophycin-52 and Pancreatic-Neoplasms

Article	Year
A convergent approach to cryptophycin 52 analogues: synthesis and biological evaluation of a novel series of fragment a epoxides and chlorohydrins. Journal of medicinal chemistry, 2003, Jul-03, Volume: 46, Issue:14 Cryptophycin 52 is a synthetic derivative of Cryptophycin 1, a potent antimicrotubule agent isolated from cyanobacteria. In an effort to increase the potency and water solubility of the molecule, a structure-activity relationship study (SAR) was initiated around the phenyl ring of fragment A. These Cryptophycin 52 analogues were accessed using a Wittig olefination reaction between various triphenylphosphonium salts and a key intermediate aldehyde prepared from Cryptophycin 53. Substitution on the phenyl ring of fragment A was well tolerated, and several of these analogues were equally or more potent than Cryptophycin 52 when evaluated in vitro in the CCRF-CEM leukemia cell line and in vivo against a murine pancreatic adenocarcinoma. Topics: Adenocarcinoma; Animals; Antineoplastic Agents; Depsipeptides; Drug Screening Assays, Antitumor; Humans; Lactams; Lactones; Male; Mice; Neoplasm Transplantation; Pancreatic Neoplasms; Structure-Activity Relationship; Tumor Cells, Cultured	2003
Synthesis and biological evaluation of novel cryptophycin analogs with modification in the beta-alanine region. Bioorganic & medicinal chemistry letters, 1999, Jan-04, Volume: 9, Issue:1 Structure modification of the beta-alanine region (fragment C) of the potent antimitotic agent cryptophycin was investigated. This includes: (1) introduction of substituents at the previously unsubstituted C7 position of the macrolide ring and (2) replacement of the (2R)-3-amino-2-methyl-propanoic acid (beta-alanine) with various (1)-amino acids to give the corresponding 15-membered unnatural cryptophycin analogs. Topics: Amino Acid Substitution; Animals; Antineoplastic Agents; beta-Alanine; Carcinoma; Colonic Neoplasms; Depsipeptides; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Humans; Mice; Models, Molecular; Pancreatic Neoplasms; Peptides, Cyclic; Protein Conformation; Structure-Activity Relationship; Tumor Cells, Cultured	1999

Article

Year

A convergent approach to cryptophycin 52 analogues: synthesis and biological evaluation of a novel series of fragment a epoxides and chlorohydrins.

Journal of medicinal chemistry, 2003, Jul-03, Volume: 46, Issue:14

Cryptophycin 52 is a synthetic derivative of Cryptophycin 1, a potent antimicrotubule agent isolated from cyanobacteria. In an effort to increase the potency and water solubility of the molecule, a structure-activity relationship study (SAR) was initiated around the phenyl ring of fragment A. These Cryptophycin 52 analogues were accessed using a Wittig olefination reaction between various triphenylphosphonium salts and a key intermediate aldehyde prepared from Cryptophycin 53. Substitution on the phenyl ring of fragment A was well tolerated, and several of these analogues were equally or more potent than Cryptophycin 52 when evaluated in vitro in the CCRF-CEM leukemia cell line and in vivo against a murine pancreatic adenocarcinoma.

Topics: Adenocarcinoma; Animals; Antineoplastic Agents; Depsipeptides; Drug Screening Assays, Antitumor; Humans; Lactams; Lactones; Male; Mice; Neoplasm Transplantation; Pancreatic Neoplasms; Structure-Activity Relationship; Tumor Cells, Cultured

2003

Synthesis and biological evaluation of novel cryptophycin analogs with modification in the beta-alanine region.

Bioorganic & medicinal chemistry letters, 1999, Jan-04, Volume: 9, Issue:1

Structure modification of the beta-alanine region (fragment C) of the potent antimitotic agent cryptophycin was investigated. This includes: (1) introduction of substituents at the previously unsubstituted C7 position of the macrolide ring and (2) replacement of the (2R)-3-amino-2-methyl-propanoic acid (beta-alanine) with various (1)-amino acids to give the corresponding 15-membered unnatural cryptophycin analogs.

Topics: Amino Acid Substitution; Animals; Antineoplastic Agents; beta-Alanine; Carcinoma; Colonic Neoplasms; Depsipeptides; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Humans; Mice; Models, Molecular; Pancreatic Neoplasms; Peptides, Cyclic; Protein Conformation; Structure-Activity Relationship; Tumor Cells, Cultured

1999