ver-52296 and Neoplasm-Metastasis

ver-52296 has been researched along with Neoplasm-Metastasis* in 1 studies

Other Studies

1 other study(ies) available for ver-52296 and Neoplasm-Metastasis

Article	Year
4-Fluoro-3',4',5'-trimethoxychalcone as a new anti-invasive agent. From discovery to initial validation in an in vivo metastasis model. European journal of medicinal chemistry, 2015, Aug-28, Volume: 101 Invasion and metastasis are responsible for 90% of cancer-related mortality. Herein, we report on our quest for novel, clinically relevant inhibitors of local invasion, based on a broad screen of natural products in a phenotypic assay. Starting from micromolar chalcone hits, a predictive QSAR model for diaryl propenones was developed, and synthetic analogues with a 100-fold increase in potency were obtained. Two nanomolar hits underwent efficacy validation and eADMET profiling; one compound was shown to increase the survival time in an artificial metastasis model in nude mice. Although the molecular mechanism(s) by which these substances mediate efficacy remain(s) unrevealed, we were able to eliminate the major targets commonly associated with antineoplastic chalcones. Topics: Animals; Antineoplastic Agents, Phytogenic; Biological Products; Cell Line, Tumor; Cell Movement; Cell Survival; Chalcones; Chick Embryo; Disease Models, Animal; Dose-Response Relationship, Drug; Drug Discovery; Female; Humans; Mice; Mice, Nude; Molecular Structure; Myocardium; Neoplasm Invasiveness; Neoplasm Metastasis; Quantitative Structure-Activity Relationship	2015

Article

Year

4-Fluoro-3',4',5'-trimethoxychalcone as a new anti-invasive agent. From discovery to initial validation in an in vivo metastasis model.

European journal of medicinal chemistry, 2015, Aug-28, Volume: 101

Invasion and metastasis are responsible for 90% of cancer-related mortality. Herein, we report on our quest for novel, clinically relevant inhibitors of local invasion, based on a broad screen of natural products in a phenotypic assay. Starting from micromolar chalcone hits, a predictive QSAR model for diaryl propenones was developed, and synthetic analogues with a 100-fold increase in potency were obtained. Two nanomolar hits underwent efficacy validation and eADMET profiling; one compound was shown to increase the survival time in an artificial metastasis model in nude mice. Although the molecular mechanism(s) by which these substances mediate efficacy remain(s) unrevealed, we were able to eliminate the major targets commonly associated with antineoplastic chalcones.

Topics: Animals; Antineoplastic Agents, Phytogenic; Biological Products; Cell Line, Tumor; Cell Movement; Cell Survival; Chalcones; Chick Embryo; Disease Models, Animal; Dose-Response Relationship, Drug; Drug Discovery; Female; Humans; Mice; Mice, Nude; Molecular Structure; Myocardium; Neoplasm Invasiveness; Neoplasm Metastasis; Quantitative Structure-Activity Relationship

2015