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Dictyostatin Analogs as Potent Microtubule Stablilizers in Cancer Therapy

Detailed Technology Description

None

*Abstract

A series of dictyostatin analogs with microtubule stabilizing activity were synthesized and examined to determine biological and biochemical structure-activity relationships. Various test methods including a high-content multiparameter fluorescence-based cellular assay were used to determine microtubule morphology, chromatin condensation, mitotic arrest and cellular toxicity. Regions of dictyostatin essential for biological activity were identified. Several analogs, particularly 6-epi-dictyostatin were shown to have the greatest microtubule stabilizing activity. These analogs were shown to be effective against paclitaxel-resistant cell lines. Applications:1) Antitumor, antineoplastic2) Antiangiogenic3) Antifungal4) Anti-inflammatory and/or immunosuppressive pharmaceutical5) Veterinary or agricultural agentsAdvantages:1) Active against paclitaxel-resistant cell lines2) High potencyStage of Development* Preclinical human tumor xenografts studies

*Principal Investigator

Name: Raghavan Balachandran, Research Associate

Department: Pharm-Pharmaceutical Science

Name: Nakyen Choy, Research Associate (formerly in Curran's

Department: Chemistry

Name: Dennis Curran, Professor

Department: Distinguished Faculty-Dietrich School of Arts and Sciences

Name: Billy Day, Professor

Department: Pharm-Pharmaceutical Science

Name: Charitha Madiraju, Graduate Student

Department: Pharm-Office of the Dean

Name: Phu Qui Nguyen

Department:

Name: Youseung Shin, Graduate Student

Department: Chemistry

Country/Region

USA