Leland Stanford Junior University

Wuhan University

Yanti University

Xuechuan Hong

Hongjie Dai

Zhen Cheng

Hao Chen

Alexander Antaris

Kai Cheng

Guangyao Lv

Jianqiao Zhang

Meng Wen

Hongbo Wang

Chunrong Qu

Jinmei Zhu

Xi Zhu

Xianming Hu

Mingmin Ding

Disclosed is a small molecule dye for use in imaging in the near-infrared window, namely between 1000 nm-1700 nm wavelength. The present dyes are also useful for photoacoustic imaging and photothermal therapy. The dyes have a structure of a D-A-D (donor-acceptor-donor) fluorescent compound core and side chains rendering the compounds water soluble and easily conjugated to hydrophilic polymers and/or targeting ligands. Further disclosed is compound, CH1055 that can be PEGylated, conjugated to a targeting ligand, or conjugated to taurine. Key steps utilized to assemble the core structure of the target included a cross-Suzuki coupling reaction, iron reduction and N-thionylaniline induced ring closure. Four carboxylic acid groups were introduced into the donor-acceptor-donor (D-A-D) type fluorescent compound to impart a certain aqueous solubility and to allow facile conjugation to targeting ligands.

Small molecule dye for molecular imaging and photothermal therapy

The present invention relates to a pyrazolo[1,5-a]pyrimidine derivative of general formula 1 and a pharmaceutically acceptable salt thereof. The present invention also relates to use of compounds of formula 1 in the preparation of an anti-tumor medicament. 

Pyrazolo[1,5-A]pyrimidine derivative and use of anti-tumor thereof

Growing community of inventors

Wuhan, China

Xuechuan Hong