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Eeyarestatin I Derivatives With Improved Aqueous Solubility

Eeyarestatin I Derivatives With Improved Aqueous Solubility

Rui Ding, Ting Zhang, Jiashu Xie, Jessica Williams, Yihong Ye, Liqiang Chen

Bioorg Med Chem Lett. 2016 Nov 1;26(21):5177-5181.

PMID: 27729187

Abstract:

Inhibition of p97 (also known as valosin-containing protein (VCP)), has been validated as a promising strategy for cancer therapy. Eeyarestatin I (EerI) blocks p97 through a novel mechanism of action and has favorable anti-cancer activities against cultured cancer cells. However, its poor aqueous solubility severely limits its in vivo applications. To circumvent this problem, we have identified EerI derivatives that possess improved aqueous solubility by introducing a single solubilizing group. These modified compounds preserved endoplasmic reticulum (ER) stress-inducing and antiproliferative activities as well as generally good in vitro metabolic properties, suggesting that these EerI derivatives could serve as candidates for further optimization.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
IAR4243153	Eeyarestatin I			Price

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