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Structure-activity Relationship Studies of Thalidomide Analogs With a Taxol-Like Mode of Action

Structure-activity Relationship Studies of Thalidomide Analogs With a Taxol-Like Mode of Action

Bulbul Pandit, Zhigen Hu, Somsundaram N Chettiar, Jennifer Zink, Zili Xiao, Jonathan P Etter, Deepak Bhasin, Pui-Kai Li

Bioorg Med Chem Lett. 2013 Dec 15;23(24):6902-4.

PMID: 24169233

Abstract:

Anti-microtubule agents such as paclitaxel and docetaxel have played an important role in the treatment of cancer for many years. Recently, a small molecule that has a taxol-like mode of action (5HPP-33) was reported. Herein, the detailed structure-activity relationship (SAR) studies of 5HPP-33 analogs that are substituted at the isoindole and phenyl rings are described. Bulky substitutions (such as di-isopropyl groups) on the phenyl ring result in the isoindole and phenyl rings being perpendicular to each other. It was found that this conformation is critical for anti-microtubule activity. These studies have provided valuable information, which will be helpful in the design of more potent analogs.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP105624860	5HPP-33		105624-86-0	Price

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