A class of sawhorse-type ruthenium(I) complexes featuring a stable CORM sphere with diverse carboxylic and amino acid derivatives were synthesized and validated as lead structures for photo-activated CO-releasing molecules (PhotoCORMs). The CO release of these CORMs was triggered by 365 nm UV irradiation. Cell viability studies indicated that 3a and 3f were non-toxic both in the dark and in UV light, making them excellent lead structures for therapeutic CORMs.