FUSARAOCHROMANONE: NEW ANALOGS AS POTENTIAL ANTICANCER AND ANTIANGIOGENIC AGENTS

Fusaraochromanone：作为潜在抗癌剂和抗血管生成剂的新类似物

• 批准号: 7381331
• 负责人: ELAHE MAHDAVIAN
• 金额: $ 2.77万
• 依托单位: LOUISIANA STATE UNIV A&M COL BATON ROUGE
• 依托单位国家: 美国
• 财政年份: 2006
• 资助国家: 美国
• 起止时间: 2006-05-01 至 2007-04-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7381331
• 关键词: FUSARAOCHROMANONE; NEW; ANALOGS; POTENTIAL; ANTICANCER

This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. The subproject and investigator (PI) may have received primary funding from another NIH source, and thus could be represented in other CRISP entries. The institution listed is for the Center, which is not necessarily the institution for the investigator. Angiogenesis is a complex biological process that controls the growth of new blood vessels in the body. Normally, angiogenesis is down-regulated in adults, with the exception of wound healing and the menstrual cycle. Aberrant angiogenesis, however, has been implicated in a variety of diseases, including cancer, arthritis, and retinopathy. The promise of anti-angiogenic agents in cancer therapy came to fruition in early 2004 with FDA approval of both Erbitux (Imclone) and Avastin (Genentech) for the treatment of metastatic colon cancer. These molecules are both monoclonal antibodies that bind to growth factors that enable cancer cells to grow towards and around tumors. Without a blood supply, tumors are unable to grow beyond 2 mm in diameter. Thus anti-angiogenesis cancer therapy is already prolonging and saving thousands of peoples lives. It would be particularly advantageous to develop small molecules that can inhibit angiogenesis with the same or greater efficacy as the proteins described above. Small molecules offer distinct advantages in that they can usually be administered orally, and they are far less costly than protein drugs. This proposal outlines an important scientific problem involving drug discovery in the field of cancer research. It targets the synthesis of a natural product, Fusarochromanone, and its novel amide analogs with potent anti-angiogenic activity. Fusarochromanone is also known to exhibit activity against a variety of cancer cell lines as well. Thus, this research could ultimately enhance our knowledge of angiogenesis and the growth factors that control both the growth of blood vessel cells and cancer cells.

该子项目是利用 NIH/NCRR 资助的中心拨款提供的资源的众多研究子项目之一。子项目和研究者 (PI) 可能已从另一个 NIH 来源获得主要资金，因此可以在其他 CRISP 条目中得到体现。列出的机构是中心的机构，不一定是研究者的机构。血管生成是一个复杂的生物过程，控制体内新血管的生长。通常，除了伤口愈合和月经周期外，成人的血管生成是下调的。然而，异常的血管生成与多种疾病有关，包括癌症、关节炎和视网膜病。 2004 年初，随着 FDA 批准 Erbitux (Imclone) 和 Avastin (Genentech) 用于治疗转移性结肠癌，抗血管生成药物在癌症治疗中的承诺得以实现。这些分子都是单克隆抗体，可与生长因子结合，使癌细胞能够向肿瘤及其周围生长。如果没有血液供应，肿瘤的直径就无法生长超过 2 毫米。因此，抗血管生成癌症治疗已经延长并挽救了数千人的生命。开发能够以与上述蛋白质相同或更强的功效抑制血管生成的小分子将是特别有利的。小分子具有独特的优势，因为它们通常可以口服给药，而且它们的成本远低于蛋白质药物。该提案概述了癌症研究领域涉及药物发现的一个重要科学问题。它的目标是合成天然产物 Fusarochromanone 及其具有有效抗血管生成活性的新型酰胺类似物。 Fusarochromanone 还具有针对多种癌细胞系的活性。因此，这项研究最终可以增强我们对血管生成以及控制血管细胞和癌细胞生长的生长因子的了解。