Bio-Organic Division, Bhabha Atomic Research Centre, Mumbai, 400085, India.
Homi Bhabha National Institute, Anushakti Nagar, Mumbai, 400094, India.
ChemMedChem. 2024 Jun 3;19(11):e202400041. doi: 10.1002/cmdc.202400041. Epub 2024 Mar 5.
Despite of having many advantages over the popular cancer therapies, photodynamic therapy still is not widely acceptable for clinical applications. Scarcity of efficient triplet photosensitizers (PSs) is one of the main bottlenecks for this. Although numerous heavy atom attached PSs are developed as PDT agents, but these are not suitable for clinical applications due to several reasons. Thus, development of heavy-atom-free organic PSs is urgently required. In this context, development of new type of helical BODIPYs as PSs for PDT is discussed. BODIPYs have rich photophysical properties and structural helicity further enhances their triplet conversion rates. This new concept of structural helicity to enhance the triplet conversion of BODIPYs is discussed with reported helical BODIPYs. Helical geometries of these dyes are checked by X-ray crystallography studies and their high triplet conversions as compared to planar BODIPYs are also confirmed. Importantly, these dyes have high triplet lifetimes and are capable of generating high singlet oxygens even in hypoxia condition as compared to conventional heavy atom attached BODIPYs. All these make the helical BODIPYs excellent candidates as PDT agents. Finally, their successful applications as PDT agents in killing of various types of cancer cells are also discussed. The results are encouraging which indicate that helical BODIPYs could be next generation heavy-atom-free PSs for PDT applications.
尽管光动力疗法相对于流行的癌症疗法有许多优势,但仍未被广泛接受用于临床应用。缺乏高效的三重态光敏剂(PS)是主要瓶颈之一。尽管已经开发了许多附着重原子的 PS 作为 PDT 试剂,但由于多种原因,这些试剂并不适合临床应用。因此,迫切需要开发无重原子的有机 PS。在这种情况下,讨论了新型螺旋 BODIPY 作为 PDT 的 PS 的发展。BODIPY 具有丰富的光物理性质,结构螺旋性进一步提高了它们的三重态转化速率。通过报道的螺旋 BODIPY 讨论了结构螺旋性增强 BODIPY 三重态转化的新概念。通过 X 射线晶体学研究检查了这些染料的螺旋几何形状,并证实了它们与平面 BODIPY 相比具有更高的三重态转化。重要的是,与传统的附着重原子的 BODIPY 相比,这些染料具有较长的三重态寿命,并且能够在缺氧条件下产生高单线态氧。所有这些都使螺旋 BODIPY 成为优秀的 PDT 试剂候选物。最后,还讨论了它们在杀死各种类型的癌细胞中的 PDT 应用的成功应用。结果令人鼓舞,表明螺旋 BODIPY 可能成为下一代 PDT 应用的无重原子 PS。