201049-37-8

Usage

Uses

Used in Anticancer Applications:
Epothilone E is utilized as an anticancer agent, specifically targeting human cancer cells that are resistant to taxane treatments. It modulates the microtubule dynamics and disrupts the normal cell division process, leading to the inhibition of tumor growth and progression. The compound's ability to overcome multidrug resistance makes it a valuable asset in the fight against cancer.
Used in Drug Delivery Systems:
To enhance the efficacy and bioavailability of Epothilone E, researchers have developed novel drug delivery systems. These systems employ various organic and metallic nanoparticles as carriers for the delivery of Epothilone E, aiming to improve its distribution, absorption, and therapeutic outcomes in cancer treatment. By optimizing the delivery of Epothilone E, these systems can potentially increase the compound's effectiveness against cancer cells and reduce side effects.

Upstream product

• 152044-53-6 epithilone A 
• 212321-22-7 4-((E)-2-((1S,3S,7S,10R,11S,12S,16R)-7,11-dihydroxy-8,8,10,12-tetramethyl-5,9-dioxo-4,17-dioxabicyclo[14.1.0]heptadecan-3-yl)prop-1-en-1-yl)-2-methylthiazole 3-oxide 
• 152044-54-7 epothilone B 
• 212321-23-8 (4-((E)-2-((1S,3S,7S,10R,11S,12S,16R)-7,11-dihydroxy-8,8,10,12-tetramethyl-5,9-dioxo-4,17-dioxabicyclo[14.1.0]-heptadecan-3-yl)prop-1-en-1-yl)thiazol-2-yl)methyl acetate 
• 204513-26-8 (Z)-(4S,7R,8S,9S,16S)-4-(tert-Butyl-dimethyl-silanyloxy)-8-hydroxy-16-((E)-2-iodo-1-methyl-vinyl)-5,5,7,9-tetramethyl-oxacyclohexadec-13-ene-2,6-dione 
• 204513-24-6 (3S,6R,7S,8S)-3-(tert-Butyl-dimethyl-silanyloxy)-7-hydroxy-4,4,6,8-tetramethyl-5-oxo-tridec-12-enoic acid (S)-1-((E)-2-iodo-1-methyl-vinyl)-but-3-enyl ester 
• 204513-16-6 (Z)-(4S,7R,8S,9S,16S)-4,8-Dihydroxy-16-((E)-2-iodo-1-methyl-vinyl)-5,5,7,9-tetramethyl-oxacyclohexadec-13-ene-2,6-dione 
• 204513-22-4 (3S,1E)-1-iodo-2-methylhexa-1,5-dien-3-ol 
• 204513-12-2 Desoxyepothilone E 

Relevant academic research and scientific papers

Characterizing the Epothilone Binding Site on β-Tubulin by Photoaffinity Labeling: Identification of β-Tubulin Peptides TARGSQQY and TSRGSQQY as Targets of an Epothilone Photoprobe for Polymerized Tubulin

Photoaffinity labeling with an epothilone A photoprobe led to the identification of the β-tubulin peptides TARGSQQY and TSRGSQQY as targets of the photoprobe for polymerized tubulin. These peptides represent residues 274-281 in different β-tubulin isotype

Epothilones C, E and F

Epothilone derivatives are obtained by: (1) cultivation of Sorangium cellulosum DSM 6773 in the presence of an absorption resin; (2) separation of the resin and culture followed by washing with aqueous methanol; (3) eluting the washed resin with methanol and reducing the extract; (4) partitioning the extract between methanol and hexane; (5) reducing the methanolic phase and fractionating it on a Sephadex column, and (6) isolation of the epothilones by chromatography using a methanol/water mixture. Epothilone A is followed by epothilone B, and two further fractions.

Epothilones with modified side chain

Epothilones with a modified side chain and process for the preparation thereof are disclosed.

Total synthesis of Epothilone E and related side-chain modified analogues via a stille coupling based strategy

A Stille coupling strategy has been utilized to complete a total synthesis of epothilone E from vinyl iodide 7 and thiazole-stannane 8h. The central core fragment 7 and its trans-isomer 11 were prepared from triene 15 using ring-closing metathesis (RCM),