ECB-ART-40496
Chem Biol Drug Des
2007 Dec 01;706:485-90. doi: 10.1111/j.1747-0285.2007.00591.x.
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In vivo evaluation of indolyl glyoxamides in the phenotypic sea urchin embryo assay.
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We have devised a ''one-pot'' phenotypic in vivo assay for the rapid evaluation of potential tubulin inhibitors using the sea urchin embryo model. An effect of a small molecule on two specific developmental stages of sea urchin embryo, namely: (i) fertilized egg test for antimitotic activity and (ii) behavioral monitoring of a free-swimming blastulae for changes in the embryo swimming pattern could be quantified by a threshold concentration resulting in respective abnormalities. Derivatives of the clinical candidate D-24851 featured good correlation between activity in tubulin polymerization assay and our in vivo data. Importantly, we demonstrated that in these series, the N-substitution of indole is non-essential to attain profound in vitro and cellular effects.
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Genes referenced: LOC100887844 tubgcp2