Tsinghua University

Institute of Nuclear Energy Research, Atomic Energy Council

Ho-Lien Huang

Chung-Shan Yu

Wuu-Jyh Lin

Jenn-Tzong Chen

Wen-Chin Su

Ching-Shiuann Yang

Shiou-Shiow Farn

Chia-Wen Huang

Yin-Cheng Huang

Shao-Wei Chen

Ying-Cheng Huang

Kun-Ju Lin

Chia-Rong Chen

Kang-Wei Chang

Shu-Fan Tien

Chun-Nan Yeh

Jia-Rong Chen

Yuan-Hsiao Su

Wei-Yuan Lee

Li-Wu Chiang

The present invention provides a method of preparing [I]Iodooctyl fenbufen amide with a radiochemical yield of 15%, a specific activity of 37 GBq/&#x3bc;mol and radiochemical purity of 95%. The present invention further provides a method of applying [I]Iodooctyl fenbufen amide as tracer of single photon emission computer tomography (SPECT) to estimate the distribution of cyclooxygenase. By the binding characteristics of the iodine isotope-labeled compounds and the positive correlation of inflammation to tumor lesion, the present invention can estimate the tumor development and metastasis.

[object Object]

A tumor radiation probe of iodine-123 marker thymidine (FLT) analogue [I]-IaraU is disclosed. Commercial available uridine is used as the raw material for the synthesis of the precursor. A radioactive iodine-123 is marked on an alkaline group of uridine to obtain [I]-IaraU, which is distinguishable from [F]-FLT markingF on a glycosyl group to obtain a novel tumor radiation probe. The marking procedures include mixing the marker precursor with Na [I] solution, acetic acid and hydrogen peroxide solution, and the solution of chloroform and sodium hydroxide. The sonication time increases from 1 minute to 10 minutes, so that [I]-IaraU has radiologically chemical purity of higher than 98% and radiological specific activity of not less than 0.196 GBq/umole, and the yield can increase from 8% to 40%. Its radioactive specific activity, yield and purity reach to the degree for the use in biological experiments, while reducing production cost.

A process for synthesizing and screening solution phase derived libraries of fenbufen and ethacrynic acid is provided in the present invention. Compounds in the present invention having cytotoxicities are useful for a variety of therapeutic applications.

Construction and screening of solution-phase derived library of fenbufen and ethacrynic acid

Growing community of inventors

Hsinchu, Taiwan

Ho-Lien Huang