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Noninvasive treatments for terminal cancer patients constitute a new trend in tumor treatment. Therefore, phototherapy, including photodynamic therapy (PDT) and photothermal therapy (PTT), has attracted considerable interest. Light and a photosensitizer (PS) are employed in both treatment methods. For PDT, the PS generates reactive oxygen species (ROS) when exposed to light, whereas for PTT, the PS generates heat. In this regard, the systematic design of new PSs has become an active area of phototherapy research in an effort to solve the problems associated with conventional PSs. In the past decade, activatable and heavy‐atom‐free PSs have become significant research areas. Therefore, we discuss our recent contributions to the PDT and PTT in this account. [ABSTRACT FROM AUTHOR]

Novel thiocarbonyl derivatives (NIS and CRNS) with excellent ROS generation abilities are synthesized and studied as potential photosensitizers for one- and two-photon excited photodynamic therapy. In particular, NIS-Me and CRNS display outstanding phototoxicity toward HeLa cells under two-photon excitation (800 nm) with negligible dark toxicity. [ABSTRACT FROM AUTHOR]

A novel sulfur-substituted naphthalimide (LSNI-S) was synthesized and investigated as a promising lysosome-targeting photosensitizer for photodynamic cancer therapy. The introduction of a dual-functional morpholine group to the 4-position of the naphthalimide backbone combined with the substitution of oxygen atoms by sulfur atoms could facilitate intersystem crossing from the excited singlet state to the reactive triplet state, leading to an excellent singlet oxygen generation efficiency of LSNI-S in organic solvents (Φ Δ ≈ 0.84 in air-saturated acetonitrile). Interestingly, LSNI-S could produce reactive oxygen species via both type-I and type-II mechanisms under physiological conditions. In particular, cell studies demonstrated that LSNI-S selectively localizes in lysosomes of cancer cells and exhibits excellent photodynamic therapy efficacy. Image 1 • A novel lysosome-targeting photosensitizer for selective photodynamic therapy was proposed. • LSNI-S could produce reactive oxygen species via both type-I and type-II mechanisms under physiological conditions. • LSNI-S exhibited excellent photodynamic therapy efficacy toward HeLa cells. [ABSTRACT FROM AUTHOR]