Frequent side effects of radical treatment modalities and the availability of novel diagnostics have raised the interest in focal therapies for localized prostate cancer. To improve the selectivity and therapeutic efficacy of such therapies, we developed a minimally invasive procedure based on a novel polymeric photosensitizer prodrug sensitive to urokinase-type plasminogen activator (uPA). The...

In light of the continued threat antimicrobial-resistant bacteria, new strategies to expand repertoire antimicrobial compounds are necessary. Prodrugs an underexploited strategy in this effort. Here, we report on enhanced activity a prodrug toward bacteria having enzyme capable its activation. A screen led us sulfurol ester antibiotic trans-3-(4-chlorobenzoyl)acrylic acid. An endogenous esteras...

Midodrine is a prodrug metabolized to the peripheral acting alpha agonist desglymidodrine and used treat orthostatic hypotension. Reports of overdose are rare, consequently there little gu...

Background Host defence peptide (HDP) has multiple properties [1,2] potentiating it as a novel anticancer agent. However disadvantages include systemic toxicity [3]. To address this, a prodrug was developed and the aim was to assess toxicity differentials between this prodrug and its active peptide component on T84 colonic carcinoma cells. Prodrug bio activation mechanism was also assessed by u...

Etodolac, a nonsteroidal antiinflammatory drug, widely used in arthritis is associated with gastric ulceration and irritation due to presence of free carboxylic group. The current investigation reports synthesis of mutual amide prodrug of etodolac by masking free carboxylic group with glucosamine, a nutritional supplement for treatment of arthritis. Confirmation and characterization of the stru...

Colchicinoids are very potent tubulin-binding compounds, which interfere with microtubule formation, giving them strong cytotoxic properties, such as cell mitosis inhibition and induction of microcytoskeleton depolymerization. While this makes them promising vascular disrupting agents (VDAs) in cancer therapy, their dose-limiting toxicity has prevented any clinical application for this purpose....

A new and selective breast cancer-targeting prodrug system is described based on the Staudinger ligation bioorthogonal reaction.

BACKGROUND: Antibody-directed enzyme prodrug therapy (ADEPT) is a promising new approach to deliver anticancer drugs selectively to tumor cells. In this approach, an enzyme is conjugated to a tumor-specific antibody. The antibody selectively localizes the enzyme to the tumor cell surface. Subsequent administration of a prodrug substrate of the enzyme leads to the enzyme-catalyzed release of the...