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Medicinal-Pharmaceutical Chemistry Commons

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Full-Text Articles in Medicinal-Pharmaceutical Chemistry

Re-Engineering Drug Discovery And Development, Garret A. Fitzgerald Oct 2011

Re-Engineering Drug Discovery And Development, Garret A. Fitzgerald

Issue Briefs

The rate of new drug approvals in the US has remained essentially constant since 1950, while the costs of drug development have soared. Many commentators question the sustainability of the current model of drug development, in which large pharmaceutical companies incur markedly escalating costs to deliver the same number of products to market. This Issue Brief summarizes the problem, describes ongoing governmental efforts to influence the process, and suggests changes in regulatory science and translational medicine that may promote more successful development of safe and effective therapeutics.


Nir-Emissive Polymersomal Markers For Molecular-Level Detection Of Metastasis, Wei Qi Aug 2011

Nir-Emissive Polymersomal Markers For Molecular-Level Detection Of Metastasis, Wei Qi

Publicly Accessible Penn Dissertations

Noninvasive imaging technologies, capable of visualizing early carcinoma or dormant or latent metastatic tumor cells and evaluating the efficacy of cancer therapies are becoming increasingly important. In this thesis, NIR-emissive polymersomes are engineered for optimal cellular uptake to enable fluorescence-based tumor targeting. A series of benzothiadiazole conjugated porphyrin oligomers with high emission dipole strength and exceptional large quantum yields in the NIR region are synthesized for optimized emissive output would be greatly enhanced. Furthermore, this thesis established for the first time a class of universal chemistry modification methods to directly attach antibody to polymersomes surface with very high antibody coupling ...


The Synthesis And Biological Evaluation Of Tamandarin B Analogs, Kenneth Lassen May 2011

The Synthesis And Biological Evaluation Of Tamandarin B Analogs, Kenneth Lassen

Publicly Accessible Penn Dissertations

The tamandarin and didemnins are a class of cyclodepsipeptides that have shown a wide range of biological activity. The didemnins have demonstrated antitumor, antiviral and immunosuppressive activity at low nano- and femtomolar levels. Didemnin B was the first marine natural product to enter clinical trials in humans in the United States. The structures of tamandarins A and B were reported in 2000 and possess almost identical structure and biological activity to didemnin B. These compounds have shown impressive biological activity and some progress has been made in establishing structure-activity relationships. However, their molecular mechanism of action is still unclear. The ...