Oxazolomycin is a new antitumor antibiotic isolated from Streptomyces sp. (Y-32026). The structural elucidation of this non-crystalline antibiotic has been carried out. Its structure has been determined as shown in 1 on the basis of spectral analysis, X-ray crystallographic analysis or synthesis of corresponding degraded products. Our interests have been focused on not only its novel structure exemplified as the β-lactone functional groupings but also the structure-activity relationship. Therefore, in vitro direct cytotoxicity of oxazole derivatives and each segment of oxazolomycin has been examined. Based on some obtained results, the structure-activity relationship of oxazolomycin will be discussed. Isolation and strcutures of two minor congeners will be also reported.
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