The next generation of synthetically-accessible anticancer drugs exist at minor c

描述（由申请人提供）：治疗癌症显然是一个非常困难的过程，虽然取得了进展，但仍有许多工作要做。许多看似有希望的化合物未能达到预期，这告诉我们必须积极地继续开发新的、创新的研究方法，以发现新的抗癌药物。第一阶段SBIR项目的目标是鉴定在未研究的植物中存在的低浓度的新型抗癌化合物，以便它们可以启发下一代抗癌药物。红杉科学是天然产品化学领域公认的领导者。红杉发表的和未发表的数据压倒性地表明，新的化学多样性存在于植物中，浓度很低，其中一些化合物很容易合成。在这项1期SBIR提案中，红杉提出了广泛纯化和去复制的色谱组分抑制人类肿瘤细胞系生长的令人信服的数据。这些数据表明，具有新的化学结构和新的抑制活性的化合物将在第一阶段的SBIR中被鉴定出来。在组合化学、基因组学和结构辅助药物设计的时代，人们很容易认为不再需要自然界中进化出来的结构多样性；然而，非常清楚的是，仅靠这些新技术无法满足迅速老龄化的美国人口的需求。药物化学家立即需要从天然产物所占据的独特化学空间中获得新的结构灵感。第一阶段SBIR提出了一个详细的计划，为药物化学家提供这种新的结构灵感。公共卫生相关性：根据NCI的数据，2008年仅美国就将有565,560人死于癌症。根据2003-2005年的比率，今天出生的人中可能有43%将被诊断出患有某种形式的癌症。治疗癌症显然是一个非常困难的过程，虽然取得了进展，但仍有许多工作要做。然而，非常清楚的是，仅靠现有的技术无法满足美国人口迅速老龄化的需求。第一阶段SBIR项目的目标是鉴定在未研究的植物中存在的低浓度的新型抗癌化合物，以便它们可以启发下一代抗癌药物。药物化学家立即需要从天然产物所占据的独特化学空间中获得新的结构灵感。

DESCRIPTION (provided by applicant): Treating cancer is clearly a very difficult process, and while progress has been made, much work remains to be done. The failures of many seemingly promising compounds to meet expectations have taught us that we must aggressively continue to develop new, innovative research methods to discover new anticancer agents. The objective of this Phase 1 SBIR project is to identify novel anticancer compounds existing at minor concentrations in unstudied plants, so that they can inspire the next generation of anticancer drugs. Sequoia Sciences is a recognized leader in natural products chemistry. Sequoia's published and unpublished data overwhelmingly suggest that new chemical diversity exists at minor concentrations in plants, and that some of these compounds are readily synthetically attainable. In this Phase 1 SBIR proposal, Sequoia presents compelling data on extensively purified and dereplicated chromatographic fractions that inhibit the growth of human tumor cell lines. These data suggest that compounds with novel chemical structures and novel inhibitory activities will be identified during this Phase 1 SBIR. In the era of combinatorial chemistry, genomics, and structure-aided drug design, it is tempting to think that the structural diversity evolved in nature is no longer needed; it has become resoundingly clear, however, that these new technologies alone will not meet the needs of the rapidly aging US population. Medicinal chemists immediately require new structural inspiration from the distinct chemical space occupied by natural products. This Phase 1 SBIR proposes a detailed plan to provide this new structural inspiration for medicinal chemists. PUBLIC HEALTH RELEVANCE: According to the NCI, 565,560 people will die from cancer in 2008 the United States alone. Based on rates from 2003-2005, it is likely that 43% of all people born today will be diagnosed with some form of cancer. Treating cancer is clearly a very difficult process, and while progress has been made, much work remains to be done. It has become resoundingly clear, however, that current technologies alone will not meet the needs of the rapidly aging US population. The objective of this Phase 1 SBIR project is to identify novel anticancer compounds existing at minor concentrations in unstudied plants, so that they can inspire the next generation of anticancer drugs. Medicinal chemists immediately require new structural inspiration from the distinct chemical space occupied by natural products.