isomigrastatin and Pancreatic-Neoplasms

isomigrastatin has been researched along with Pancreatic-Neoplasms* in 1 studies

Other Studies

1 other study(ies) available for isomigrastatin and Pancreatic-Neoplasms

ArticleYear
Synthesis of Migrastatin Analogues as Inhibitors of Tumour Cell Migration: Exploring Structural Change in and on the Macrocyclic Ring.
    Chemistry (Weinheim an der Bergstrasse, Germany), 2015, Dec-07, Volume: 21, Issue:50

    Migrastatin and isomigrastatin analogues have been synthesised in order to contribute to structure-activity studies on tumour cell migration inhibitors. These include macrocycles varying in ring size, functionality and alkene stereochemistry, as well as glucuronides. The synthesis work included application of the Saegusa-Ito reaction for regio- and stereoselective unsaturated macroketone formation, diastereoselective Brown allylation to generate 9-methylmigrastatin analogues and chelation-induced anomerisation to vary glucuronide configuration. Compounds were tested in vitro against both breast and pancreatic cancer cell lines and inhibition of tumour cell migration was observed in both wound-healing (scratch) and Boyden chamber assays. One unsaturated macroketone showed low affinity for a range of secondary drug targets, indicating it is at low risk of displaying adverse side effects.

    Topics: Alkenes; Cell Line, Tumor; Cell Movement; Female; Glucuronides; Humans; Macrocyclic Compounds; Macrolides; Pancreatic Neoplasms; Piperidones; Structure-Activity Relationship

2015