Structural highlights
8ahm is a 6 chain structure with sequence from Bos taurus, Gallus gallus and Rattus norvegicus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
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| Ligands: | , , , , , , , , |
| Resources: | FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT |
Function
E1BQ43_CHICK
Publication Abstract from PubMed
We describe the total synthesis of the macrodiolide C(13)/C(13')-bis(desmethyl)disorazole Z via double inter-/intramolecular Stille cross-coupling of a monomeric vinyl stannane/vinyl iodide precursor to achieve macrocycle formation. The key step in the synthesis of this precursor was a stereoselective aldol reaction of a formal Evans acetate aldol product with crotonaldehyde. As demonstrated by X-ray crystallography, the binding mode of C(13)/C(13')-bis(desmethyl)disorazole Z to tubulin is virtually identical with that of the natural product disorazole Z. Likewise, C(13)/C(13')-bis(desmethyl)disorazole Z inhibits tubulin assembly with at least the same potency as disorazole Z and it appears to be a more potent cell growth inhibitor.
Synthesis and Biological Evaluation of C(13)/C(13')-Bis(desmethyl)disorazole Z.,Bold CP, Lucena-Agell D, Oliva MA, Diaz JF, Altmann KH Angew Chem Int Ed Engl. 2022 Oct 25. doi: 10.1002/anie.202212190. PMID:36281761[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Bold CP, Lucena-Agell D, Oliva MA, Diaz JF, Altmann KH. Synthesis and Biological Evaluation of C(13)/C(13')-Bis(desmethyl)disorazole Z. Angew Chem Int Ed Engl. 2022 Oct 25. doi: 10.1002/anie.202212190. PMID:36281761 doi:http://dx.doi.org/10.1002/anie.202212190
