Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Structure-Activity Relationships among Zygosporin Derivatives
湊 均片山 照明松本 誠片桐 謙松浦 真三砂川 則雄堀 賢司原田 稔竹内 三津男
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1973 年 21 巻 10 号 p. 2268-2277

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Cytochalasin D (zygosporin A) showed strong cytotoxic effect with a unique cytopathogenic change. Further, cytochalasin D inhibited the growth of several rat tumors in a narrow chemotherapeutic index range owing to its irritating toxicity. More than 30 derivatives of zygosporin were synthesized, and structure-biology relationship was discussed for cytotoxicity and skin irritating activity. Among the derivatives, cytochalasin C has similar cytotoxicity to cytochalasin D, accompanied by a decreased lethal toxicity. It is disappointing, however, that the chemotherapeutic index of cytochalasin C is no different from that of cytochalasin D.
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© The Pharmaceutical Society of Japan
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