Course synthesis of active site directed oncolytic agents

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dc.contributor.committeeMemberWilliams, Louis
dc.contributor.committeeMemberCates, Lindley A.
dc.contributor.committeeMemberMartin, Gary E.
dc.contributor.committeeMemberSmith, Lewis K.
dc.contributor.committeeMemberSapp, John B., Jr.
dc.contributor.committeeMemberParker, George R.
dc.creatorMahayni, Muhamed Madhat
dc.date.accessioned2022-09-23T19:25:17Z
dc.date.available2022-09-23T19:25:17Z
dc.date.issued1977
dc.description.abstractA unique approach in obtaining new synthetic anticancer compounds involves the chelation of trace metals associated with cancer cells. Several α-(N)-heterocyclic carboxaldehyde thiosemicarbazones (HCT), with the potential to form coordination compounds with certain transition metals inhibit the growth of a number of transplanted rodent neoplasms, spontaneous lymphomas of dogs, and DNA viruses of the Herpes family. Several researchers have investigated the structure activity relationship of HCT compounds and found the activity was best with 5-amino-1-formyl-thiosemicarbazone isoquinoline. The objective of this investigation was to explore the principle of active site-directed drug design. This principle has been utilized to develop very potent drugs, for example dilantin and amino sugars like 2-amino-3-ß-D-glucose, which have been used as a carrier of nitrogen mustard. Applying this principle, an attempt has been made to generate a model antitumor agent which would be more potent and be delivered more specifically to the site of action than previously existing antitumor agents. Hence, one of the most active chelators in clinical trial, 5-amino-1-formylisoquinoline thiosemicarbazone was modified by attaching at position five one of the essential amino acids as a carrier, preferably L-phenylalanine. The synthesis of other thiosemicarbazone analogs were also attempted.
dc.description.departmentPharmacy, College of
dc.format.digitalOriginreformatted digital
dc.format.mimetypeapplication/pdf
dc.identifier.other3831211
dc.identifier.urihttps://hdl.handle.net/10657/12058
dc.language.isoen
dc.rightsThis item is protected by copyright but is made available here under a claim of fair use (17 U.S.C. Section 107) for non-profit research and educational purposes. Users of this work assume the responsibility for determining copyright status prior to reusing, publishing, or reproducing this item for purposes other than what is allowed by fair use or other copyright exemptions. Any reuse of this item in excess of fair use or other copyright exemptions requires express permission of the copyright holder.
dc.titleCourse synthesis of active site directed oncolytic agents
dc.type.dcmiText
dc.type.genreThesis
thesis.degree.collegeCollege of Pharmacy
thesis.degree.departmentPharmacy, College of
thesis.degree.disciplinePharmacy
thesis.degree.grantorUniversity of Houston
thesis.degree.levelMasters
thesis.degree.nameMaster of Science

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