A10: SYNTHESIS OF NON NUCLEOSIDIC ANTIVIRAL AGENTS: HIV & CANCER DRUG DESIGN

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The design, synthesis and evaluation of antiviral agents of the non-nucleosidic type remain the major goal of this research project. Our lead compound 2,3-diveratryl-3-chloropropenal (compound 1) and active antiviral agent serves as a starting point for structural activity relationships. (SAR) for drug design. Compound 1 contains the alpha, beta unsaturated carbonyl group in its molecular structure. We used this unsaturated carbonyl group as a combinational starting point for new medicinal entities. Chalcones the un-cyclic precursor to flavonoids, contain the alpha, beta unsaturated carbonyl group in its chemical structure. Chalcones have been shown to express antiproliferative activity by a number of investigators. Leinamycin, an antibiotic with antitumor activity, contains an extended unsaturated (alpha, beta, gamma, delta) carbonyl group in its chemical structure. Although a significant amount of antitumor activity is associated with the 1,2 diethylene-3-oxide group of the leinamycin molecule, it cannot account for all of its antitumor action. We suggest that the alpha, beta, gamma, delta unsaturated carbonyl group also contributes to leinamycin antitumor activity.