与碳环α,β-和β,γ-稠合的γ-内酯作为新型抗增殖药物。
Gamma-lactones alpha,beta- and beta,gamma-fused to carbocycles as novel antiproliferative drugs.
作者信息
León Leticia G, Machín Rubén P, Rodríguez Carmen M, Ravelo José L, Martín Víctor S, Padrón José M
机构信息
Instituto Universitario de Bio-Orgánica Antonio González, Universidad de La Laguna, C/Astrofísico Francisco Sánchez 2, 38206 La Laguna, Spain.
出版信息
Bioorg Med Chem Lett. 2008 Oct 1;18(19):5171-3. doi: 10.1016/j.bmcl.2008.08.098. Epub 2008 Aug 29.
A set of gamma-lactones alpha,beta-fused and beta,gamma-fused to carbocycles have been synthesized and evaluated for their in vitro antiproliferative activities using the human cancer cell lines SW1573 (lung), T-47D (breast) and WiDr (colon). The compounds are obtained by intramolecular ring closing metathesis of the corresponding dienes. Active compounds exhibited GI(50) values in the range 8-18 microM. A structure-activity relationship is also discussed.
已合成了一组与碳环α,β-稠合和β,γ-稠合的γ-内酯，并使用人癌细胞系SW1573（肺癌）、T-47D（乳腺癌）和WiDr（结肠癌）评估了它们的体外抗增殖活性。这些化合物通过相应二烯的分子内环化复分解反应获得。活性化合物的GI(50)值在8-18 microM范围内。还讨论了构效关系。
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