A facile synthesis of deaza-analogues of the bisindole marine alkaloid topsentin.

A facile synthesis of deaza-analogues of the bisindole marine alkaloid topsentin.
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Bisindole海洋生物碱topsentin的Deaza-Analogues的便捷合成。

DOI:
10.3390/molecules18032518
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发表时间:
2013-02-26
期刊:
Molecules (Basel, Switzerland)
影响因子:
--
通讯作者:
Favi G
Favi G
中科院分区:
其他
文献类型:
--
作者:
Carbone A;Spanò V;Parrino B;Ciancimino C;Attanasi OA;Favi G

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A series of substituted ethyl 1-[(tert-butoxycarbonyl)amino]-2-methyl-5-(1-methyl-1H-indol-3-yl)-4-[(1-methyl-1H-indol-3-yl)carbonyl]-1H-pyrrole-3-carboxylates were prepared in excellent yields (82-98%) by one-pot reactions between β-dicarbonyl compounds 12a–e and 1,2-diaza-1,3-diene (DD) 13. Derivatives 10a,c–e, deazaanalogues of the bis-indole alkaloid topsentin, screened by the National Cancer Institute (Bethesda, MD, USA) in the in vitro one dose primary anticancer assay against a panel of about 60 human tumor cell lines, showed no significant activity, with the exception of compound 9e, which showed moderate activity against the HOP-92 cell line of the non small cell lung cancer sub-panel and the SNB-75 cell line of the CNS sub-panel.
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