Antitumor compounds based on a natural product consensus pharmacophore

Antitumor compounds based on a natural product consensus pharmacophore
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DOI:
10.1021/jm8006195
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发表时间:
2008-10-09
影响因子:
7.3
通讯作者:
Webb, Thomas R.
Webb, Thomas R.
中科院分区:
医学1区
文献类型:
--
作者:
Lagisetti, Chandraiah;Pourpak, Alan;Webb, Thomas R.

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We report the design and highly enantioselective synthesis of a potent analogue of the spliceosome inhibitor FR901464, based on a non-natural product scaffold. The design of this compound was facilitated by a pharmacophore hypothesis that assumed key interaction types that are common to FR901464 and an otherwise unrelated natural product (pladienolide). The synthesis allows for the preparation of numerous novel analogues. We present results on the in vitro activity for this compound against several tumor cell lines.