cycloproparadicicol and Breast-Neoplasms

cycloproparadicicol has been researched along with Breast-Neoplasms* in 2 studies

Other Studies

2 other study(ies) available for cycloproparadicicol and Breast-Neoplasms

Article	Year
New efficient synthesis of resorcinylic macrolides via ynolides: establishment of cycloproparadicicol as synthetically feasible preclinical anticancer agent based on Hsp90 as the target. Journal of the American Chemical Society, 2004, Jun-30, Volume: 126, Issue:25 A program currently ongoing in our laboratory envisions natural macrolide radicicol-based inhibitors targeting the molecular chaperone Hsp90. Such inhibitors can be potential anticancer agents due to their ability to induce the breakdown of a variety of oncogenic proteins. In this account, we first concern ourselves with a vastly important total synthesis of such an inhibitor. We accomplished this via a new approach, which we term the "ynolide method", directed to the synthesis of resorcinylic macrolides, including cycloproparadicicol and aigialomycin D. The key features of the syntheses involve cobalt-complexation-promoted ring-closing metathesis (RCM) to generate ynolides, followed by Diels-Alder reaction with dimedone-derived bis-siloxy dienes to elaborate the benzo system. A number of interesting analogues were synthesized using this protocol. They were evaluated for their inhibitory activity against the growth of breast cancer cell line, MCF-7. The potency of their cytotoxicity was found to be consistent with their ability to degrade the oncogenic protein, Her2. From these assays, cycloproparadicicol was identified as a most promising candidate for further development. Topics: Antineoplastic Agents; Breast Neoplasms; Cell Line, Tumor; Cobalt; Cyclopropanes; HSP90 Heat-Shock Proteins; Humans; Inhibitory Concentration 50; Lactones; Macrolides; Molecular Chaperones; Molecular Structure; Resorcinols	2004
Total synthesis as a resource in the discovery of potentially valuable antitumor agents: cycloproparadicicol. Angewandte Chemie (International ed. in English), 2003, Mar-17, Volume: 42, Issue:11 Topics: Antineoplastic Agents; Breast Neoplasms; Cell Division; Cyclopropanes; Drug Design; HSP90 Heat-Shock Proteins; Humans; Inhibitory Concentration 50; Lactones; Macrolides; Molecular Structure; Protein Binding; Structure-Activity Relationship; Tumor Cells, Cultured	2003

Article

Year

New efficient synthesis of resorcinylic macrolides via ynolides: establishment of cycloproparadicicol as synthetically feasible preclinical anticancer agent based on Hsp90 as the target.

Journal of the American Chemical Society, 2004, Jun-30, Volume: 126, Issue:25

A program currently ongoing in our laboratory envisions natural macrolide radicicol-based inhibitors targeting the molecular chaperone Hsp90. Such inhibitors can be potential anticancer agents due to their ability to induce the breakdown of a variety of oncogenic proteins. In this account, we first concern ourselves with a vastly important total synthesis of such an inhibitor. We accomplished this via a new approach, which we term the "ynolide method", directed to the synthesis of resorcinylic macrolides, including cycloproparadicicol and aigialomycin D. The key features of the syntheses involve cobalt-complexation-promoted ring-closing metathesis (RCM) to generate ynolides, followed by Diels-Alder reaction with dimedone-derived bis-siloxy dienes to elaborate the benzo system. A number of interesting analogues were synthesized using this protocol. They were evaluated for their inhibitory activity against the growth of breast cancer cell line, MCF-7. The potency of their cytotoxicity was found to be consistent with their ability to degrade the oncogenic protein, Her2. From these assays, cycloproparadicicol was identified as a most promising candidate for further development.

Topics: Antineoplastic Agents; Breast Neoplasms; Cell Line, Tumor; Cobalt; Cyclopropanes; HSP90 Heat-Shock Proteins; Humans; Inhibitory Concentration 50; Lactones; Macrolides; Molecular Chaperones; Molecular Structure; Resorcinols

2004

Total synthesis as a resource in the discovery of potentially valuable antitumor agents: cycloproparadicicol.

Angewandte Chemie (International ed. in English), 2003, Mar-17, Volume: 42, Issue:11

Topics: Antineoplastic Agents; Breast Neoplasms; Cell Division; Cyclopropanes; Drug Design; HSP90 Heat-Shock Proteins; Humans; Inhibitory Concentration 50; Lactones; Macrolides; Molecular Structure; Protein Binding; Structure-Activity Relationship; Tumor Cells, Cultured

2003