Epothilone A

Epothilone A Structure
Epothilone A structure
Common Name Epothilone A
CAS Number 152044-53-6 Molecular Weight 493.656
Density 1.1±0.1 g/cm3 Boiling Point 683.3±55.0 °C at 760 mmHg
Molecular Formula C26H39NO6S Melting Point 95ºC
MSDS Chinese USA Flash Point 367.1±31.5 °C

Identifying off-target effects and hidden phenotypes of drugs in human cells.

Nat. Chem. Biol. 2 , 329-37, (2006)

We present a strategy for identifying off-target effects and hidden phenotypes of drugs by directly probing biochemical pathways that underlie therapeutic or toxic mechanisms in intact, living cells. High-content protein-fragment complementation assays (PCAs)...

Neuronal transcriptional repressor REST suppresses an Atoh7-independent program for initiating retinal ganglion cell development.

Dev. Biol. 349 , 90-9, (2011)

As neuronal progenitors differentiate into neurons, they acquire a unique set of transcription factors. The transcriptional repressor REST prevents progenitors from undergoing differentiation. Notably, REST binding sites are often associated with retinal gang...

Conformational preferences of natural and C3-modified epothilones in aqueous solution.

J. Med. Chem. 51 , 1469-73, (2008)

The conformational properties of the microtubule-stabilizing agent epothilone A ( 1a) and its 3-deoxy and 3-deoxy-2,3-didehydro derivatives 2 and 3 have been investigated in aqueous solution by a combination of NMR spectroscopic methods, Monte Carlo conformat...

Cyclostreptin binds covalently to microtubule pores and lumenal taxoid binding sites.

Nat. Chem. Biol. 3 , 117-25, (2007)

Cyclostreptin (1), a natural product from Streptomyces sp. 9885, irreversibly stabilizes cellular microtubules, causes cell cycle arrest, evades drug resistance mediated by P-glycoprotein in a tumor cell line and potently inhibits paclitaxel binding to microt...

Synthesis and biological evaluation of epothilone A dimeric compounds

Bioorg. Med. Chem. 17 , 7435-40, (2009)

The preparation and biological evaluation of a novel series of dimeric epothilone A derivatives (1-6) are described. Two types of diacyl spacers were introduced to establish the various dimeric epothilone A constructs. The effect of these compounds on tubulin...

Synthesis and SAR of C12-C13-oxazoline derivatives of epothilone A.

Bioorg. Med. Chem. Lett. 19 , 3760-3, (2009)

The SAR of a series of new epothilone A derivatives with a 2-substituted-1,3-oxazoline moiety trans-fused to the C12-C13 bond of the deoxy macrocycle have been investigated with regard to tubulin polymerization induction and cancer cell growth inhibition. Sig...

Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry.

J. Med. Chem. 48 , 5613-38, (2005)