MEK-5, a member of the MAPK family, phosphorylates ERK-5 permitting cells to survive oxidative stress. MEK-5 is upregulated in tumor cells and activated by mitogens; inhibition of this enzyme is a potential anti-cancer strategy. Scaffolds from the following classes--benzimidazole, diphenylamine, flavones, and ortho-carboxyamide were examined for their capacity to be developed into potent and selective MEK-5 inhibitors.
Tubulysin is a natural product that disrupts microtubule dynamics, blocks mitosis, and induces cell death. It has been examined as a potential anti-cancer agent in hollow fiber assays. Simple and reliable procedures were developed for the gram-scale synthesis of Mep-Ile dipeptide and Tup fragments of tubulysin.","abstract_html":"CDK-5 is associated with hyperphosphorylation of the microtubule-associated protein tau, formation of neurofibrillary tangles, and possibly an acceleration of the neurodegenerative progression of Alzheimer's disease. C6-O linked benzimidazoles and C-4 benzamide and phenylacetamide benzimidazoles based on (R)-Roscovitine, a non-selective inhibitor of CDK-5 were designed and synthesized. </p><p>MEK-5, a member of the MAPK family, phosphorylates ERK-5 permitting cells to survive oxidative stress. MEK-5 is upregulated in tumor cells and activated by mitogens; inhibition of this enzyme is a potential anti-cancer strategy. Scaffolds from the following classes--benzimidazole, diphenylamine, flavones, and ortho-carboxyamide were examined for their capacity to be developed into potent and selective MEK-5 inhibitors. </p><p>Tubulysin is a natural product that disrupts microtubule dynamics, blocks mitosis, and induces cell death. It has been examined as a potential anti-cancer agent in hollow fiber assays. Simple and reliable procedures were developed for the gram-scale synthesis of Mep-Ile dipeptide and Tup fragments of tubulysin.","abstract_has_math":false,"creators":["Chopra, Ishveen Kaur"],"institution":null,"degree_name":"MS","degree_level":"Immediate Access","degree_discipline":"Medicinal Chemistry","degree_department":null,"school":null,"contributors":["Patrick Flaherty","Aleem Gangjee","Marc Harrold","David Lapinsky","Jane Cavanaugh"],"advisors":[],"committee_chairs":[],"committee_members":[],"year":2010,"date_issued":"2010-01-01T08:00:00Z","date_published":"2010-01-01T08:00:00Z","updated_at":"2026-07-24T02:09:27Z","subjects":["Benzimidazoles","Diphenylamine","Flavones","MEK-5","Ortho-Carboxyamide","Tubulysin"],"languages":["English"],"rights":[],"rights_urls":[],"identifier_entries":[]},"links":{"outbound_url":"https://dsc.duq.edu/etd/404","outbound_label":"Repository record","outbound_source":"dc:identifier"},"metadata_groups":[{"id":"people","label":"People","entries":[{"key":"dc:contributor","label":"Contributor","values":["Patrick Flaherty","Aleem Gangjee","Marc Harrold","David Lapinsky","Jane Cavanaugh"]},{"key":"dc:creator","label":"Author","values":["Chopra, Ishveen Kaur"]}]},{"id":"academic_context","label":"Academic Context","entries":[{"key":"dc:date.available","label":"Dc Date Available","values":["2018-08-03T07:00:00Z"]},{"key":"thesis:degree_discipline","label":"Discipline","values":["Medicinal Chemistry"]},{"key":"thesis:degree_level","label":"Degree Level","values":["Immediate Access"]},{"key":"thesis:degree_name","label":"Degree Name","values":["MS"]}]},{"id":"subjects_keywords","label":"Subjects and Keywords","entries":[{"key":"dc:subject","label":"Dc Subject","values":["Benzimidazoles","Diphenylamine","Flavones","MEK-5","Ortho-Carboxyamide","Tubulysin"]}]},{"id":"language_rights","label":"Language and Rights","entries":[{"key":"dc:language","label":"Dc Language","values":["English"]}]},{"id":"identifiers","label":"Identifiers","entries":[{"key":"dc:identifier","label":"Identifier","values":["https://dsc.duq.edu/etd/404"]}]},{"id":"additional","label":"Additional Metadata","entries":[{"key":"dc:description.abstract","label":"Abstract","values":["CDK-5 is associated with hyperphosphorylation of the microtubule-associated protein tau, formation of neurofibrillary tangles, and possibly an acceleration of the neurodegenerative progression of Alzheimer's disease. C6-O linked benzimidazoles and C-4 benzamide and phenylacetamide benzimidazoles based on (R)-Roscovitine, a non-selective inhibitor of CDK-5 were designed and synthesized.
MEK-5, a member of the MAPK family, phosphorylates ERK-5 permitting cells to survive oxidative stress. MEK-5 is upregulated in tumor cells and activated by mitogens; inhibition of this enzyme is a potential anti-cancer strategy. Scaffolds from the following classes--benzimidazole, diphenylamine, flavones, and ortho-carboxyamide were examined for their capacity to be developed into potent and selective MEK-5 inhibitors.
Tubulysin is a natural product that disrupts microtubule dynamics, blocks mitosis, and induces cell death. It has been examined as a potential anti-cancer agent in hollow fiber assays. Simple and reliable procedures were developed for the gram-scale synthesis of Mep-Ile dipeptide and Tup fragments of tubulysin."]},{"key":"dc:title","label":"Title","values":["Design and Synthesis of CDK-5 and MEK-5 Inhibitors and Synthesis towards Tubulysin Analogs"]}]}],"canonical_facts":{"dc:contributor":["Patrick Flaherty","Aleem Gangjee","Marc Harrold","David Lapinsky","Jane Cavanaugh"],"dc:creator":["Chopra, Ishveen Kaur"],"dc:date.available":["2018-08-03T07:00:00Z"],"dc:description.abstract":["CDK-5 is associated with hyperphosphorylation of the microtubule-associated protein tau, formation of neurofibrillary tangles, and possibly an acceleration of the neurodegenerative progression of Alzheimer's disease. C6-O linked benzimidazoles and C-4 benzamide and phenylacetamide benzimidazoles based on (R)-Roscovitine, a non-selective inhibitor of CDK-5 were designed and synthesized.
MEK-5, a member of the MAPK family, phosphorylates ERK-5 permitting cells to survive oxidative stress. MEK-5 is upregulated in tumor cells and activated by mitogens; inhibition of this enzyme is a potential anti-cancer strategy. Scaffolds from the following classes--benzimidazole, diphenylamine, flavones, and ortho-carboxyamide were examined for their capacity to be developed into potent and selective MEK-5 inhibitors.
Tubulysin is a natural product that disrupts microtubule dynamics, blocks mitosis, and induces cell death. It has been examined as a potential anti-cancer agent in hollow fiber assays. Simple and reliable procedures were developed for the gram-scale synthesis of Mep-Ile dipeptide and Tup fragments of tubulysin."],"dc:identifier":["https://dsc.duq.edu/etd/404"],"dc:language":["English"],"dc:subject":["Benzimidazoles","Diphenylamine","Flavones","MEK-5","Ortho-Carboxyamide","Tubulysin"],"dc:title":["Design and Synthesis of CDK-5 and MEK-5 Inhibitors and Synthesis towards Tubulysin Analogs"],"thesis:degree_discipline":["Medicinal Chemistry"],"thesis:degree_level":["Immediate Access"],"thesis:degree_name":["MS"]},"updated_at":"2026-07-24T02:09:27Z"}