temozolomide-selenium analog

Temozolomide-selenium (TMZ-Se) is a synthetic analog of the alkylating agent temozolomide, designed to enhance antitumor activity and overcome resistance mechanisms in cancers such as malignant glioma and melanoma. Developed by researchers at Penn State University, the molecule features an N-ethylselenocyanate extension attached to the amide functionality of the temozolomide core. This modification allows the drug to function as a more potent DNA alkylator while simultaneously inducing higher levels of apoptosis and autophagy compared to the parent compound. Notably, TMZ-Se exhibits a stronger down-regulating effect on O6-methylguanine-DNA methyltransferase (MGMT), an enzyme that typically confers resistance to alkylating agents by repairing DNA damage. Preclinical data indicates that TMZ-Se is effective against TMZ-resistant cell lines and demonstrates superior tumor-inhibiting activity in xenograft models.

Other names

temozolomide-seleniumN-ethylselenocyanate-temozolomide