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ChemInform Abstract: Alkyl Esters of Camptothecin and 9-Nitrocamptothecin: Synthesis, in vitro Pharmacokinetics, Toxicity, and Antitumor Activity.

✍ Scribed by Z. CAO; N. HARRIS; A. KOZIELSKI; D. VARDEMAN; J. S. STEHLIN; B. GIOVANELLA

Publisher: John Wiley and Sons
Year: 2010
Weight: 29 KB
Volume: 29
Category: Article
ISSN: 0931-7597
DOI: 10.1002/chin.199818232

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✦ Synopsis

Alkyl Esters of Camptothecin and 9-Nitrocamptothecin: Synthesis, in vitro Pharmacokinetics, Toxicity, and Antitumor Activity.

-Eleven title esters (I) are synthesized to evaluate their biological properties in comparison with those of their parent compounds camptothecin and 9nitrocamptothecin. Especially esters (Ia) and (Id) exhibit significant antitumor activity combined with little or no toxicity in vivo. Furthermore, in vitro pharmacokinetic evaluation shows that the biological life span of their closed lactone form is significantly increased in comparison to their parent compounds.

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