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

抗病毒药物的设计、合成及评价 非核苷型仍然是本研究项目的主要目标。 我们的先导化合物2，3-二恶基-3-氯丙酚(化合物1)和 活性抗病毒药物是结构性治疗的起点 活动关系。(SAR)用于药物设计。化合物1包含 其分子结构中的α，β不饱和羰基。 我们用这个不饱和的羰基作为组合的开始 为新的医疗实体加分。查尔酮--非循环前体 对于类黄酮类，含有α，β不饱和羰基 它的化学结构。查尔康斯已经被证明可以表达 一些研究人员的抗增殖活性。雷那霉素， 一种具有抗肿瘤活性的抗生素，含有一种扩展的 其化学成分中的不饱和(α、β、伽马、三角洲)羰基 结构。尽管有大量的抗肿瘤活性 与雷诺霉素的1，2-二乙基-3-氧基有关 分子，它不能解释其所有的抗肿瘤作用。我们 提示α、β、伽马、三角洲不饱和羰基 也有助于雷诺霉素的抗肿瘤活性。

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.