Bioorganic & medicinal chemistry

Fluorescent phosphoinositide 3-kinase inhibitors suitable for monitoring of intracellular distribution

D Kim, H Lee, H Jun, SS Hong, S Hong

Index: Kim, Donghee; Lee, Hyunseung; Jun, Hwiseok; Hong, Soon-Sun; Hong, Sungwoo Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 8 p. 2508 - 2516

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Citation Number: 9

Abstract

Abstract The monitoring of the drug behavior and distribution in biological system can provide information whether drug reaches its desired target, and a biological rationale for the design of new therapeutics. We have developed a family of potent fluorescent PI3Kα inhibitors in which part of the fluorophore was engineered to be a pharmacophore capable of inhibiting PI3Kα. These xanthine derivatives are characterized by a donor–acceptor ...