Discovery of a New Class of Antitumor Agents
Dartmouth researchers have synthesized a novel class of antitumor agents. These potential new drugs were designed to bind more tightly to cancer cell DNA than many conventional anticancer drugs by a process called bis-intercalation or "double-binding," much like a molecular staple. Such binding stops the growth of the cancer cell and it dies.
Improving upon the concept of bis-intercalation, the Dartmouth chemists have utilized a unique semi-rigid tether connecting the two intercalating units which greatly increases the energy of binding and prevents the undesirable "self-stacking" of the drug, which had been observed previously and would decrease or render inert its efficacy. This semi-rigid tether was designed to allow the twin intercalating rings to adapt to the contours of the helical DNA for maximum bis-intercalation.
Given the problem of cancer chemotherapeutic drug resistance, it is essential to develop new drugs with new and more powerful modes of action. Following more extensive development, these newly developed bis-intercalators offer a promising new class of agent for the treatment of cancer.
This technology is claimed in the issued United States Patent No. 6,187,787. We are seeking an industrial partner interested in its commercialization. (Ref: J47)
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