Rational Design of New Anti-cancer Drug
DescriptionMitochondria-targeting drugs have received extensive interest for decades due to the vital roles of mitochondria in regulating energy metabolism and governing programmed cell death. Consequently, engineering cell permeable drug carriers capable of targeting this crucial organelle for drug action is under active development. In this regard, drug functionalization with tripheoylphosphonium (TPP) has been demonstrated to increase drug accumulation and retention in mitochondria. Despite these advantages, introducing TPP group to metallodrugs is not straight forward. We propose to synthesize new air and moisture stable phosphonium ring-fused metallacycles as a new type of anti-cancer drug through activation of terminal ynones. Preliminary results show that these metallacycles possess mitochondrial-accumulating ability, and exhibit stronger cytotoxicity against several common human cancer cell lines compared with their corresponding metal precursors and the classic anticancer agent cisplatin.
|Effective start/end date||1/09/19 → …|