2066-88-8Relevant articles and documents
Synthesis of Migrastatin Analogues as Inhibitors of Tumour Cell Migration: Exploring Structural Change in and on the Macrocyclic Ring
LoRe, Daniele,Zhou, Ying,Mucha, Joanna,Jones, Leigh F.,Leahy, Lorraine,Santocanale, Corrado,Krol, Magdalena,Murphy, Paul V.
, p. 18109 - 18121 (2015)
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.
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Lawes,B.C.
, p. 6413 - 6414 (1960)
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Synthesis and antiviral activities of synthetic glutarimide derivatives
Ji, Xing-Yue,Zhong, Zhao-Jin,Xue, Si-Tu,Meng, Shuai,He, Wei-Ying,Gao, Rong-Mei,Li, Yu-Huan,Li, Zhuo-Rong
experimental part, p. 1436 - 1441 (2010/12/25)
A series of novel glutarimide compounds were synthesized and their antiviral activities were evaluated. The compounds displaying the strongest antiviral activities included 5, 6f, 7e and 9 against coxsackievirus B3 (Cox B3), 10 and 6f against influenza vi
MIGRASTATIN ANALOG COMPOSITIONS AND USES THEREOF
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Page 180, (2010/02/08)
In one aspect, the present invention provides pharmaceutical compositions comprising a therapeutically effective amount of a compound of general formula (I), wherein R1-R6, Ra-RC, Q, Y1, Y2 and n are as defined herein, whereby the composition is formulated for administration to a subject at a dosage between about 0.1 mg/kg to about 50 mg/kg of body weight. In another aspect, the present invention provides a method for treating breast tumor metastasis in a subject comprising administering to a subject in need thereof a therapeutically effective amount of the inventive composition described directly above and a pharmaceutically acceptable carrier, adjuvant or vehicle.