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Quinaldine based semisquaraines and squaraine dyes, process for preparation thereof and use thereof

机译:喹诺丁类半方酸和方酸类染料,其制备方法及其用途

摘要

The present invention provides quinaldine-based semisquaraines, symmetrical and unsymmetrical squaraine dyes represented by the general formulae 1, 2 and 3 and/or pharmaceutically acceptable derivatives thereof as sensitizers for photodynamic therapeutical and industrial applications. These symmetrical and unsymmetrical squaraine dyes posses absorption which extends well into the photodynamic window (650-800 nm) and hence are useful for the treatment of deep seated tumors. The absorption of these dyes can be tuned by changing the substituents on the quinaldine moiety thereby enabling the development of a library of dyes which have absorption ranging from 650 to 800 nm. They also exhibited fluorescence emission in the long wavelength region making them useful as near infrared fluorescence sensors for the detection of tumors. These dyes are non-toxic in the dark and exhibit good photocytotoxicity. Accordingly the quinaldine based semisquaraines, symmetrical and unsymmetrical squaraines are extremely useful as diagnostic and therapeutic agents for photodynamic therapeutical and industrial applications.
机译:本发明提供了由通式1、2和3表示的基于喹诺定的半方酸,对称和非对称方酸染料和/或其药学上可接受的衍生物,作为用于光动力治疗和工业应用的敏化剂。这些对称和不对称的方酸染料具有良好的吸收能力,该吸收能力很好地延伸到光动力窗口(650-800 nm)内,因此可用于治疗深部肿瘤。这些染料的吸收可以通过改变奎纳啶部分上的取代基来调节,从而能够开发吸收范围为650至800 nm的染料库。它们还在长波长区域显示出荧光发射,使其可用作检测肿瘤的近红外荧光传感器。这些染料在黑暗中无毒,并具有良好的光细胞毒性。因此,基于喹纳丁的半方胺,对称和不对称方胺作为光动力治疗和工业应用的诊断和治疗剂非常有用。

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