[show abstract][hide abstract] ABSTRACT: Recurrent prostate cancer (PCa) remains a major clinical challenge. Invasive and metastatic PCa lesions often exhibit a partial and time-limited response to therapy before the cancer progresses and the patient succumbs to the disease. Despite recent advances in early diagnosis and treatment, approximately one-third of treated patients will relapse and become resistant to currently available treatments. In this review we evaluate current treatment practices and recent advances in therapy for localized prostate malignancy and advanced, metastatic prostate cancer. Some of the promising new drugs for PCa treatment include MDV3100, an androgen receptor (AR) antagonist that prevents androgens from binding to the AR and nuclear translocation and co-activator recruitment of the ligand-receptor complex; abiraterone, an orally administered drug that irreversibly inhibits a rate-limiting enzyme in androgen biosynthesis, CYP17; and several newer cytotoxic drugs (epothilones, satraplatin). Key new insights are that cancer stem cells play a role in PCa and that PCa cells are dependent on the AR for proliferation, even in the hormone refractory state of the disease. We also discuss potential molecular targets for new drug candidates for the treatment of metastatic PCa.
Current Medicinal Chemistry 08/2011; 18(29):4440-53. · 4.07 Impact Factor
[show abstract][hide abstract] ABSTRACT: [reaction: see text]. (+)-Galiellalactone was synthesized starting from (R)-(+)-pulegone. Natural and synthetic galiellalactone have opposite optical rotations, demonstrating that the structure of the natural product is 1a.
[show abstract][hide abstract] ABSTRACT: Coprinol, a new antibacterial cuparane, was isolated from fermentations of a Coprinus sp. Its biological activities were investigated and its structure was elucidated by spectroscopic methods. The new antibiotic exhibited activitiy against multidrug-resistant Gram-positive bacteria in vitro. Two derivatives were synthesized and their activities compared to the parent compound.
Zeitschrift fur Naturforschung C 01/2001; 56(1-2):31-4. · 0.60 Impact Factor
[show abstract][hide abstract] ABSTRACT: The three protoilludanes radulone A (1), radulone B (2) and radudiol (3), the illudalane radulactone (4) and the illudane radulol (5) were isolated from the extracts of the culture fluids of the basidiomycete Radulomyces confluens. The structures of the five new compounds were determined by spectroscopic techniques. Radulone A (1) is a potent inhibitor of human and bovine platelet aggregation stimulated by different agonists, inhibiting preferentially the aggregation of human platelets induced by ADP with an IC50 value of 2 microM. In addition 1 exhibits cytotoxic and antimicrobial activities. The other four compounds exhibited weak antimicrobial and cytotoxic activity.
Zeitschrift fur Naturforschung C 01/1998; 53(11-12):939-45. · 0.60 Impact Factor