Rhodamine derivatives for photodynamic therapy of cancer and in vitro
purging of the leukemias
    10.
    发明授权

    公开(公告)号:US5773460A

    公开(公告)日:1998-06-30

    申请号:US674247

    申请日:1996-07-01

    CPC分类号: C07D311/82 A61K41/0057

    摘要: The present invention relates to novel photoactivable rhodamine derivatives for enhancing high quantum-yield production and singlet oxygen generation upon irradiation with light while maintaining desirable differential retention of rhodamine between normal and cancer cells. Representative derivatives are 2-(4,5-dibromo-6-amino-3-imino-3H-xanthen-9-yl)-benzoic acid methyl ester hydrochloride; 2-(4, 5-dibromo-6-amino-3-imino-3H-xanthen-9-yl)-benzoic acid ethyl ester hydrochloride; 2-(4,5-dibromo-6-amino-3-imino-3H-xanthen-9-yl)-benzoic acid octyl ester hydrochloride; 2-(4,5-dibromo-6-amino-3-imino-3H-xanthen-9-yl)-benzoic acid n-butyl ester hydrochloride; 2-(6-ethyl amino-3-ethyl imino-3H-xanthen-9-yl)-benzoic acid n-butyl ester hydrochloride; and photoactivable derivatives thereof. These derivatives are utilized in an amount to achieve appropriate intracellular levels of the derivative when irradiation of a suitable wavelength and intensity is applied to photoactivate the derivative and thereby induce cell killing.

    摘要翻译: 本发明涉及用于在照射光时提高高量子产率产生和单线态氧产生的新型可光致发光罗丹明衍生物,同时保持罗丹明在正常癌细胞与癌细胞之间的期望差异保留。 代表性的衍生物是2-(4,5-二溴-6-氨基-3-亚氨基-3H-呫吨-9-基) - 苯甲酸甲酯盐酸盐; 2-(4,5-二溴-6-氨基-3-亚氨基-3H-呫吨-9-基) - 苯甲酸乙酯盐酸盐; 2-(4,5-二溴-6-氨基-3-亚氨基-3H-呫吨-9-基) - 苯甲酸辛酯盐酸盐; 2-(4,5-二溴-6-氨基-3-亚氨基-3H-呫吨-9-基) - 苯甲酸正丁酯盐酸盐; 2-(6-乙基氨基-3-乙基亚氨基-3H-呫吨-9-基) - 苯甲酸正丁酯盐酸盐; 和其可光活化的衍生物。 当照射适当的波长和强度以光激活衍生物并由此诱导细胞杀伤时,这些衍生物用量达到适当的细胞内水平的衍生物。