Advances in the discovery of kinesin spindle protein (Eg5) inhibitors as antitumor agents.

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El-Nassan HB

Advances in the discovery of kinesin spindle protein (Eg5) inhibitors as antitumor agents.

Eur J Med Chem. 2013 Apr;62:614-31. doi: 10.1016/j.ejmech.2013.01.031. Epub 2013 Feb 5.

PubMed ID

23434636 [ View in PubMed

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Abstract

Cancer is considered as one of the most serious health problems. Despite the presence of many effective chemotherapeutic agents, their severe side effects together with the appearance of mutant tumors limit the use of these drugs and increase the need for new anticancer agents. Eg5 represents an attractive target for medicinal chemists since Eg5 is overexpressed in many proliferative tissues while almost no Eg5 is detected in nonproliferative tissues. Many Eg5 inhibitors displayed potent anticancer activity against some of the mutant tumors with limited side effects. The present review provides an overview about the progress in the discovery of Eg5 inhibitors especially from 2009 to 2012 as well as the clinical trials conducted on some of these inhibitors.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
[(4R)-4-(3-HYDROXYPHENYL)-1,6-DIMETHYL-2-THIOXO-1,2,3,4-TETRAHYDROPYRIMIDIN-5-YL](PHENYL)METHANONE	Kinesin-like protein KIF11	IC 50 (nM)	110	N/A	N/A	Details
[(4R)-4-(3-HYDROXYPHENYL)-1,6-DIMETHYL-2-THIOXO-1,2,3,4-TETRAHYDROPYRIMIDIN-5-YL](PHENYL)METHANONE	Kinesin-like protein KIF11	IC 50 (nM)	150	N/A	N/A	Details
Monastrol	Kinesin-like protein KIF11	IC 50 (nM)	30000	N/A	N/A	Details