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Medicinal and Pharmaceutical Chemistry

Virginia Commonwealth University

1981

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Synthesis And Biological Evaluation Of Sparsomycin Analogues, Scherer Preston Sanders Jan 1981

Synthesis And Biological Evaluation Of Sparsomycin Analogues, Scherer Preston Sanders

Theses and Dissertations

In 1962, Owen, Dietz, and Camiener reported the isolation of a new antitumor antibiotic from the culture filtrate of Streptomyces sparsogenes. The structure of the crystalline antibiotic, named sparsomycin, remained elusive until 1970, when Wiley and MacKellar reported results of spectroscopic and degradation studies which elucidated the structure. In addition to the molecular structure, investigators have examined the mechanism of action, toxicity, and related analogues, striving to establish sparsomycin or a synthetic analogue's usefulness as an effective chemotherapeutic agent.

The initial pharmacological evaluation of sparsomycin revealed it possessed activity against KB human epidermoid carcinoma cells, a variety of gram-negative and …