Cancer is one of the deadly diseases affecting significant percentage of population throughout the world. cancers are categorized by the type of cells that are affected initially and over 100 different types of cancers are known. owing to the increasing number of deaths and difficulties associated in the treatment of cancer, several therapeutic techniques have been implemented by the researchers working in this field. presently, chemotherapy, surgery, radiation therapy, etc., are routinely used mode of treatments given to the patients, although there are some disadvantages associated with them. one such limitation is that the repeated chemotherapeutic dose given to a patient leads to serious side effects and eventually makes them immune to the drug. therefore, there is an immediate requirement of a suitable therapeutic modality, which does not lead to any side effects and is non-invasive so that the malignancy can be controlled. photodynamic therapy (pdt) is one of the non-invasive techniques, which involves localized activation of drug by irradiation of light of certain wavelength. however, such a treatment has been only considered effective for the treatment of superficial cancers. although photofrin® is a clinically-approved drug having spatial and temporal control in the mode of action, it has several limitations. photofrin® decomposes to form bilirubin and biliverdin, leading to jaundice. furthermore, patients treated with photofrin® can become sensitive towards visible light. to overcome such shortcomings, metal-based complexes may serve as better targets to treat cancer. there are several advantages in using metal complexes as they have versatile coordination geometry and they can involve in photo-redox pathways for the generation of reactive oxygen species (ros) to kill cancer cells. combination of different units such as photosensitizer and targeting molecule can be conjugated together, thus enhancing the efficacy. in this regard, our approach was to prepare iron(iii) complex. iron is a bio-relevant metal and it is present in 30-40 mg quantity per kg body weight. therefore, we have prepared and characterized benzhydroxamate (bha) iron(iii) complexes and evaluated their photocytotoxicity in the visible (400–700 nm) and red (600–720 nm) light. this complex exhibits preferential localization in the mitochondria. most importantly, the complex shows photocytotoxicity in red light in hela cancer cells, resulting in ic50 value of 24.4(±0.4) μm. interestingly, it is worthwhile to mention that this complex is non-toxic under dark condition, indicating the lead role of photoactivation to kill cancer cells. further studies show that the complex is localized in nucleus and mitochondria, where it produces ros upon irradiation. the most significant fact observed in this investigation is that the mode of cell death is apoptosis, which is absent in cancer cells. therefore, our investigation highlights the potential use of such bio-relevant metal complexes as effective pdt agent.