Radiolytic activation of a cytarabine prodrug possessing a 2-oxoalkyl group: one-electron reduction and cytotoxicity characteristics.

Radiolytic activation of cytarabine prodrug possessing 2-oxoalkyl group: one-electron reduction and cytotoxicity characteristics

Radiolytic Reduction Characteristics of Artificial Oligodeoxynucleotides Possessing 2-Oxoalkyl Group or Disulfide Bonds

A number of advances have been made in the development of modified oligodeoxynucleotides (ODNs), and chemical or physical properties of which are controlled by external stimuli. These intelligent ODNs are promising for the next generation of gene diagnostics and therapy. This paper focuses on the molecular design of artificial ODNs that are activated by X-irradiation and their applications to r...

Preclinical Development Molecular and Cellular Pharmacology of the Hypoxia-Activated Prodrug TH-302

TH-302 is a 2-nitroimidazole triggered hypoxia-activated prodrug (HAP) of bromo-isophosphoramide mustard currently undergoing clinical evaluation. Here, we describe broad-spectrum activity, hypoxiaselective activation, and mechanism of action of TH-302. The concentration and time dependence of TH-302 activation was examined as a function of oxygen concentration, with reference to the prototypic...

Molecular and cellular pharmacology of the hypoxia-activated prodrug TH-302.

TH-302 is a 2-nitroimidazole triggered hypoxia-activated prodrug (HAP) of bromo-isophosphoramide mustard currently undergoing clinical evaluation. Here, we describe broad-spectrum activity, hypoxia-selective activation, and mechanism of action of TH-302. The concentration and time dependence of TH-302 activation was examined as a function of oxygen concentration, with reference to the prototypi...

Lysosomal Oxidative Stress Cytotoxicity Induced by Dacarbazine and It’s Pyridine Derivative in Hepatocytes

     Dacarbazine (DTIC) is a synthetic chemical antitumor agent which is used to treat malignant melanoma and Hodgkin’s disease. DTIC is a prodrug which is converted to an active form undergoing demethylation by liver enzymes. The active form prevents the progress of disease via alkylation of DNA strand. In the structure of this drug, the imidazole ring, a triazen chain and carboxamide group ex...