基于带正电的芳香磺酰胺取代的二苯并噻唑方针菁SQ，设计并合成了五种正电性磺酰胺取代的二苯并噻唑方针菁SQ-D1~5。通过形成正电化合物、加入强电子吸引基团（-CN）来获得更高的刚性结构和完美的光敏剂SQ-D2。在所有磺酰氨方针菁中，SQ-D2化合物显示出最高的ROS产生效率和光稳定性，同时表现出最高的光细胞毒性（IC50 = 0.25±0.08μM），非常低的黑暗细胞毒性和出色的细胞摄取能力。在动物研究中，它不仅显示出有效的肿瘤保留和易于从体内排出，而且在低剂量药物（0.15mg/kg）的情况下还表现出有效的PDT疗效和良好的生物相容性。此外，相比临床批准的光敏剂m-THPC和含有光敏剂的某些纳米材料，作为单一组分的光敏剂SQ-D2在针对人类乳腺癌的PDT治疗中具有更大的潜力。这项工作为开发理想的方针菁染料光敏剂提供了新的视角。版权所有©2023 Elsevier B.V.。

On the base of the zwiterionic dibenzothiazole squaraine SQ, five cationic aromatics sulfonamide substituted dibenzothiazole squaraines SQ-D1 ∼ 5 have been designed and synthesized. Through the formation of the cationic compound, a higher rigid structure and the addition of the strong electron-withdrawing group (-CN), an ideal photosensitizer SQ-D2 has been gotten. In all the sulfonaminosquaraines, compound SQ-D2 exhibited the highest ROS generation efficacy and photostability. It also showed the highest photo-cytotoxicity (IC50 = 0.25 ± 0.08 μM), very low dark-cytotoxicity and the excellent cell uptake. In animal study, it not only showed the effective tumor retention and the easy removal from the body, but also exhibited the effective PDT efficacy at low drug dose (0.15 mg/kg) and the good biocompatibility. Furthermore, photosensitizer SQ-D2 as a single component exhibited greater potential than clinically approved photosensitizer m-THPC and some nanomaterials with photosensitizers in PDT therapy towards human breast cancer. This work provides a new perspective to develop the ideal photosensitizer of the squaraine dyes.Copyright © 2023 Elsevier B.V. All rights reserved.