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Breast Cancer Drug Discovery with Combinatorial Chemical Libraries.

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Annual rept. 2 Sep 96-1 Sep 97

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HE GOAL OF THIS PROJECT IS TO DISCOVER NEW DRUGS THAT HAVE SPECIFICITY AND SIGNIFICANT ANTICANCER ACTIVITY AGAINST BREAST CANCER. The approach uses several novel aspects that permit high volume screening for drug discovery. To maximize the number of unique chemical compounds available for testing, we have employed the new technology of combinatorial chemistry to produce large libraries containing thousands of compounds using the one-bead, one compound technology in which a portion of each compound can be released in vitro in a semisolid agarose culture of breast cancer and other tumor types as controls 1-3. During the past year we have screened three large libraries and discovered one lead compound that showed specificity against two breast cancer cell lines as compared to the control tumor types. Analogs of this lead compound have subsequently been tested and one discrete compound was found to be active in vitro at the micromolar level. This compound is currently undergoing preliminary evaluation of mechanism of action and will also be advanced to in vivo study in mice. During the coming year we will study additional large libraries in search of other lead compounds.

Subject Categories:

  • Medicine and Medical Research
  • Pharmacology
  • Inorganic Chemistry

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