Jerome Horwitz, one of Wayne State University's and Barbara Ann Karmanos Cancer Institute's (KCI) most esteemed researchers, has created an exciting anti-tumor series, the SH80 series, recently licensed to Sanofi-Synthelabo, a multi-national pharmaceutical company headquartered in Paris, France with operations in New York City and Malvern, Pennsylvania.

Horwitz, nationally recognized as the creator of AZT and two other leading therapeutics for AIDS and HIV, began searching for improved derivatives of XK469, 2-[4-(7-chloro-2-quinoxalinyloxy) phenoxy]propionic acid, originally synthesized at DuPont in 1991. Since then, he and a team of researchers at KCI, including Dr. Stuart Hazeldine and Dr. Lisa Polin have synthesized and tested an additional 125 distinct analogs of XK469. One of these, SH80, was found to be significantly more active when tested in mice.

All of the analogs synthesized were evaluated in vitro to determine cytotoxicity against leukemias and tumors. Selected in vitro active analogs were then tested in mice against various tumors. Tumors tested included pancreatic adenocarcinoma-03, colon tumor 26, and mammary adenocarcinoma-17/Adr.

After extensive testing and comparison of the analogs to XK469, SH80 was deemed superior against all three tumor types tested. Horwitz commented that even though the SH80 series shows promise, there is a tremendous rate of failure in drug discoveries. "We are cautiously optimistic on the potential effects of this compound," said Dr. Horwitz. Further testing is necessary, with drug trials potentially starting in approximately 24 months. "We will continue to look at SH80 to gain an understanding of the mechanism of how it works." If the compound proves to be safe and effective, a new anti-tumor drug may be on the market in six years or so.

"At 84, Dr. Horwitz is one of the oldest recipients ever of a five-year grant from the National Institutes of Health National Cancer Institute," commented Fred Reinhart, WSU's assistant vice president for Research and Technology Commercialization. Working under this five-year grant titled "Optimization of XK469 Against Transplanted Solid Tumors," awarded in early 2000, Horwitz and his research team discovered the SH-80 series. At 84 years young, Horwitz comes in to work everyday and finds his current work "challenging and as a whole new career." He contemplates a possible retirement at the end of his five-year grant in 2005.

Sanofi-Synthelabo is a major global research-based pharmaceutical group with 32,500 employees in more than 100 countries. The company is headquartered in Paris and listed in Paris (Euronext: SAN) and in New York (NYSE: SNY). With annual sales in excess of $8 billion, Sanofi-Synthelabo ranks 7th in Europe and among the world's top 20 pharmaceutical companies.

Sanofi-Synthelabo's core therapeutic areas are cardiovascular disease and thrombosis, diseases of the central nervous system, cancer and internal medicine. The foundation of their worldwide growth stems from their highly regarded research and development program, with about 50 compounds under development, half of which are in Phase II and Phase III clinical trials.

Wayne State University is one of the nation's pre-eminent public research universities in an urban setting. In the past 20 years, Wayne State's research has grown 11 percent annually, with research expenditures reaching nearly $170 million in 2001. Over 65 percent of research at WSU is focused on the life sciences, and this focus has led our School of Medicine to climb the National Science Foundation rankings to 23 in 2000.

Through its multidisciplinary approach to research and education, and its ongoing collaboration with government, industry and other institutions, the university seeks to enhance economic growth and improve the quality of life in the city of Detroit, state of Michigan and throughout the world.