Correlation of biologic data with physico-chemical properties among the vinca alkaloids and their congeners. |
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Authors: | R J Owellen D W Donigian C A Hartke F O Hains |
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Institution: | The Oncology Center, The Johns Hopkins University School of Medicine, Baltimore, MD 21205, U.S.A. |
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Abstract: | Displacement of 3H]vinblastine binding to tubulin by other Vinca alkaloid derivatives has been demonstrated to be a competitive process, allowing for determination of the association constant of each drug. Correlation of LD50 data and anti-P-388 activity was found with log P and log Ka, according to the equations: . Vincristine and desacetylvinblastine were the two most active agents in this series. That the latter drug had significant biologic activity was of considerable interest, since it is known to be a human metabolite. |
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