Boron neutron capture therapy (BNCT) has attracted earnest efforts and interest from both academia and the pharmaceutical industry in recent years due to its high potential in clinical applications. Following the latest development and popularization of neutron sources in China, BNCT is expected to play more important roles in cancer treatment in China. The FDA approved compounds, 4-borono-L-phenylalanine (BPA) and sodium borocaptate (BSH) (Na2B12H11SH), are currently in clinical trials but neither has fully achieved the tumor selectivity required for BNCT treatment, i.e., with less accumulation in normal tissues and/or blood. The development of a boron drug that meets all the requirements of BNCT thus remains a challenge. This lecture summarizes the syntheses of boron analogues of a-amino acid-based agents and their unique efficacy in anti-tumor and anti-rheumatoid arthritis through boron neutron capture therapy.
Dr. Yinghuai Zhu received his PhD degree from Nankai University in 1997 and then stayed on as an assistant/associate professor while also working as a postdoctoral fellow in Northern Illinois University. In 2002, he joined the Institute of Chemical and Engineering Sciences (ICES), A*STAR, Singapore as a senior research fellow. After 14 years there, followed by a brief stint as a visiting scientist back at Northern Illinois University, he joined the Macau University of Science and Technology. Since 2020, he has been with Sunshine Lake Pharma as an expert in new drug R&D. His research interests include new generation anti-cancer and anti-infective drugs such as in boron neutron capture therapy, and new nanocomposites as high efficiency catalysts in green chemistry and energy research. He has published more than 85 papers with a total citation count of more than 3300, twelve book chapters, and he holds three patents.