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Full-Text Articles in Medicine and Health Sciences
Synthesis And Antiproliferative Activities Of Doxorubicin Thiol Conjugates And Doxorubicin-Ss-Cyclic Peptide, Shaban Darwish, Neda Sadeghiani, Shirley Fong, Saghar Mozaffari, Parinaz Hamidi, Thimanthi Withana, Sun Yang, Rakesh Kumar Tiwari, Keykavous Parang
Synthesis And Antiproliferative Activities Of Doxorubicin Thiol Conjugates And Doxorubicin-Ss-Cyclic Peptide, Shaban Darwish, Neda Sadeghiani, Shirley Fong, Saghar Mozaffari, Parinaz Hamidi, Thimanthi Withana, Sun Yang, Rakesh Kumar Tiwari, Keykavous Parang
Pharmacy Faculty Articles and Research
Myocardial toxicity and drug resistance caused by drug efflux are major limitations of doxorubicin (Dox)-based chemotherapy. Dox structure modification could be used to develop conjugates with an improved biological profile, such as antiproliferative activity and higher cellular retention. Thus, Dox thiol conjugates, Dox thiol (Dox-SH), thiol-reactive Dox-SS-pyridine (SS = disulfide), and a Dox-SS-cell-penetrating cyclic peptide, Dox-SS-[C(WR)4K], were synthesized. Dox was reacted with Traut's reagent to generate Dox-SH. The thiol group was activated by the reaction with dithiodipyridine to afford the corresponding Dox-SS-Pyridine (Dox-SS-Pyr). A cyclic cell-penetrating peptide containing a cysteine residue [C(WR)4K] was prepared using Fmoc solid-phase strategy. Dox-SS-Py was …
Potent And Potentially Non-Cardiotoxic Anthracyclines: Their Synthesis, Biological Evaluation, And Comparison Of Hydrozone-Mediated Reductions, Jerrett Holdaway
Potent And Potentially Non-Cardiotoxic Anthracyclines: Their Synthesis, Biological Evaluation, And Comparison Of Hydrozone-Mediated Reductions, Jerrett Holdaway
Boise State University Theses and Dissertations
After nearly half a century since medical approval, the anthracycline doxorubicin (DOX) remains one of the most potent and clinically useful anticancer agents. In spite of its long history, however, the cytotoxic mechanisms of DOX have been debated and remain controversial. Several well-supported mechanisms will be discussed, such as the potential to intercalate DNA and induce apoptosis through topoisomerase poisoning, free radical formation, and DNA cross-linking. While DOX has substantial medical importance, it is plagued by a life-threatening dose-dependent cardiotoxic side effect associated with several structural groups. A number of modifications to DOX have been accomplished to attempt to remove …
Drug Delivery With Light, Patrick S. Dupart
Drug Delivery With Light, Patrick S. Dupart
Theses and Dissertations
Cancer is responsible for about 25% of deaths in developed countries and for 15% of all deaths worldwide. Cancer is a devastating disease and while there have been great advances in the development of anticancer drugs, off-target toxicity is a major limitation with conventional cancer chemotherapy. The consequence of this form of treatment results in the killing of healthy and rapidly-growing non-cancerous cells including cells in the bone marrow; hair follicles; and cells in the mouth, digestive tract, and reproductive system. In addition to these general effects, certain anticancer drugs can have other associated toxicities. For instance, the anticancer drug …