Discovery and development of sesquiterpenoid derived hydroxymethylacylfulvene: a new anticancer drug.
Hydroxymethylacylfulvene (HMAF, MGI 114) is derived from the sesquiterpene illudin S by treatment with dilute sulfuric acid and excess paraformaldehyde. It is less cytotoxic than illudin S but exhibits much greater selectivity in toxicity to malignant cells compared to normal cells. HMAF is believed to undergo bioreductive activation in vivo. It is now being tested in human clinical phase II trials against solid tumors.
McMorris
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Department of Chemistry and Biochemistry, University of California, San Diego, La Jolla 92093, USA.
D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000737:chemistry*; D002986:Clinical Trials as Topic; D006801:Humans; D008297:Male; D051379:Mice; D008956:Models, Chemical; D011471:Prostatic Neoplasms / Q000188:drug therapy; D051381:Rats; D012717:Sesquiterpenes / Q000138:chemical synthesis* / Q000737:chemistry*; D013678:Technology, Pharmaceutical; D014407:Tumor Cells, Cultured
D000903:Antibiotics, Antineoplastic; D012717:Sesquiterpenes; C102714:irofulven