PYRROMETHENE BORON DIFLUORIDES IN PDT

PDT 中的吡咯甲撑二氟化硼

• 批准号: 3493465
• 负责人: Lee ROY MORGAN
• 金额: $ 5万
• 依托单位: DEKK-TEC, INC.
• 依托单位国家: 美国
• 财政年份: 1993
• 资助国家: 美国
• 起止时间: 1993-07-01 至 1993-12-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3493465
• 关键词: antineoplastics; boron; chemical substitution; cytotoxicity; disease /disorder model; drug administration routes; drug design /synthesis /production; drug metabolism; growth inhibitors; heterocyclic compounds; laboratory mouse; laboratory rat; lasers; liposomes; metal complex; neoplasm /cancer photoradiation therapy; photochemistry; photosensitizing agents; singlet oxygen; tissue /cell culture; ureter; urinary tract neoplasms

The overall objective of this SBIR proposal is to develop new anticancer agents which are cytotoxic in photodynamic therapy (PDT). It has been shown by Morgan and Boyer that pyrromethene boron difluoride (P-BF2) complexes can offer this property. In Phase I, substituted (P-BF2) complexes will be prepared, characterized and evaluated for PDT potentials. Studies have documented that human ovarian cancer cells (LS-2) cultured with the disodium salt of pentamethylpyrromethene-2, 6-disulfonate boron difluoride (PMPDS-BF2) plus exposure to light produced cell growth inhibition. In addition, when PMPDS-BF2 was injected intratumor into the DMBA-rat breast cancer model, followed by exposure to quartz lamp irradiation, 50-100% tumor remissions occurred. Cyano, bistetramethylene and acetoxymethyl substituted P-BF2 complexes will be evaluated in vitro and in vivo in mouse and rat tumor models. The P-BF complexes are considered to be quasiaromatic electron impoverished (QA-eI) heterocycles. They show high extinction coefficients, high fluorescent quantum yields: those with superior laser action poses little to no triplet-triplet absorption in the fluorescence spectral region. These properties will be considered and attempts to associate them to PDT will be made.

该SBIR提案的总体目标是开发新的抗癌 在光动力疗法（PDT）中具有细胞毒性的药物。 它一直 摩根和博耶（Morgan and Boyer 复合物可以提供此属性。 在第一阶段，将准备取代（P-BF2）复合物，表征 并评估PDT电位。 研究已经记录了人类 用卵巢癌细胞（LS-2）用二钠盐培养 五甲基丙烯-2，6-二硫酸硼硼difuoride（PMPDS-BF2） 加上暴露于光产生的细胞生长抑制。 此外， 当PMPDS-BF2被注入肿瘤内DMBA乳腺癌 模型，然后接触石英灯照射，肿瘤50-100％ 发生了减免。 氰基，双甲基和乙酰氧基甲基 取代的P-BF2复合物将在体外和体内评估 小鼠和大鼠肿瘤模型。 P-BF复合物被认为是 甲状腺电子贫困（QA-EI）杂环。 他们表现得很高 灭绝系数，高荧光量子产率： 上级激光动作几乎没有呈现三胞胎 - 三曲线的吸收 荧光光谱区域。 这些特性将被考虑 并将尝试将它们与PDT关联。