{"id":{"repo_id":"cagliari","oai_identifier":"oai:iris.unica.it:11584/266708"},"canonical_url":"https://search.dev.ndltd.org/etd/cagliari/oai:iris.unica.it:11584/266708","repository":{"repo_id":"cagliari","name":"Università di Cagliari","base_url":"https://iris.unica.it/oai/request"},"display":{"title":"Design and synthesis of new potential anticancer agents and high-selective A2B antagonists","abstract":"The synthesis of antitumor agents covers a large part of current medicinal chemistry efforts. This thesis mainly focuses on the synthesis of different scaffolds as new potential anticancer agents. Two different approaches were applied: a hybrid concept and a rational based drug design. In the first case, the hybrid concept is useful since it allows combining multiple active scaffolds in a unique molecule. As a consequence, several targets could be hit simultaneously, making this solution particularly attractive for multi-factorial diseases like cancer. Within this category, several isatin-thiazolinone-pyrazoline hybrids were synthesized. Some of them were submitted to biological assays, demonstrating good activity toward different solid tumour cell-lines. In the second class of compounds, the synthetic efforts were combined to computational tools in order to achieve detailed information about the structure-activity relationships. Following this approach, psoralen derivatives, thought as DNA G-quadruplex stabilizers, were synthesized. For these compounds no biological assays were performed so far. Finally, the last part of the thesis has been dedicated to the synthesis of 1-alkyl-8-(piperazine-1-sulphonyl)phenyl xanthines as high-selective A2B antagonists. Even though the leading role of adenosine and their receptors in cancer pathogenesis were extensively documented, the high therapeutic potential of these compounds requires a wider analysis of their pharmacological properties. Also in this case, several compounds were synthesized. Some of them were tested in a radioligand binding assay to evaluate the affinity and selectivity toward A2BR subtype, further confirming the high potential of these compounds as A2B antagonists.","abstract_html":"The synthesis of antitumor agents covers a large part of current medicinal chemistry efforts. This thesis mainly focuses on the synthesis of different scaffolds as new potential anticancer agents. Two different approaches were applied: a hybrid concept and a rational based drug design. In the first case, the hybrid concept is useful since it allows combining multiple active scaffolds in a unique molecule. As a consequence, several targets could be hit simultaneously, making this solution particularly attractive for multi-factorial diseases like cancer. Within this category, several isatin-thiazolinone-pyrazoline hybrids were synthesized. Some of them were submitted to biological assays, demonstrating good activity toward different solid tumour cell-lines. In the second class of compounds, the synthetic efforts were combined to computational tools in order to achieve detailed information about the structure-activity relationships. Following this approach, psoralen derivatives, thought as DNA G-quadruplex stabilizers, were synthesized. For these compounds no biological assays were performed so far. Finally, the last part of the thesis has been dedicated to the synthesis of 1-alkyl-8-(piperazine-1-sulphonyl)phenyl xanthines as high-selective A2B antagonists. Even though the leading role of adenosine and their receptors in cancer pathogenesis were extensively documented, the high therapeutic potential of these compounds requires a wider analysis of their pharmacological properties. Also in this case, several compounds were synthesized. Some of them were tested in a radioligand binding assay to evaluate the affinity and selectivity toward A2BR subtype, further confirming the high potential of these compounds as A2B antagonists.","abstract_has_math":false,"creators":["ARRIDU, ANTONELLA"],"institution":"Università degli Studi di Cagliari","degree_name":null,"degree_level":null,"degree_discipline":null,"degree_department":null,"school":null,"contributors":[],"advisors":[],"committee_chairs":[],"committee_members":[],"year":2016,"date_issued":"2016-03-24","date_published":"2016-03-24","updated_at":"2026-07-24T01:30:12Z","subjects":["anticancer","antitumorali","design","progettazione","sintesi","synthesis","Settore CHIM/08 - Chimica Farmaceutica"],"languages":["eng"],"rights":["info:eu-repo/semantics/openAccess","license:Non specificato"],"rights_urls":[],"identifier_entries":[]},"links":{"outbound_url":"http://hdl.handle.net/11584/266708","outbound_label":"Handle","outbound_source":"dc:identifier"},"metadata_groups":[{"id":"people","label":"People","entries":[{"key":"dc:creator","label":"Author","values":["ARRIDU, ANTONELLA"]}]},{"id":"academic_context","label":"Academic Context","entries":[{"key":"dc:date","label":"Dc Date","values":["2016-03-24"]},{"key":"dc:publisher","label":"Institution","values":["Università degli Studi di Cagliari"]},{"key":"dc:relation","label":"Dc Relation","values":["numberofpages:122"]},{"key":"dc:type","label":"Dc Type","values":["info:eu-repo/semantics/doctoralThesis"]}]},{"id":"subjects_keywords","label":"Subjects and Keywords","entries":[{"key":"dc:subject","label":"Dc Subject","values":["anticancer","antitumorali","design","progettazione","sintesi","synthesis","Settore CHIM/08 - Chimica Farmaceutica"]}]},{"id":"language_rights","label":"Language and Rights","entries":[{"key":"dc:language","label":"Dc Language","values":["eng"]},{"key":"dc:rights","label":"Dc Rights","values":["info:eu-repo/semantics/openAccess","license:Non specificato"]}]},{"id":"identifiers","label":"Identifiers","entries":[{"key":"dc:identifier","label":"Identifier","values":["http://hdl.handle.net/11584/266708"]}]},{"id":"additional","label":"Additional Metadata","entries":[{"key":"dc:description","label":"Description","values":["The synthesis of antitumor agents covers a large part of current medicinal chemistry efforts. This thesis mainly focuses on the synthesis of different scaffolds as new potential anticancer agents. Two different approaches were applied: a hybrid concept and a rational based drug design. In the first case, the hybrid concept is useful since it allows combining multiple active scaffolds in a unique molecule. As a consequence, several targets could be hit simultaneously, making this solution particularly attractive for multi-factorial diseases like cancer. Within this category, several isatin-thiazolinone-pyrazoline hybrids were synthesized. Some of them were submitted to biological assays, demonstrating good activity toward different solid tumour cell-lines. In the second class of compounds, the synthetic efforts were combined to computational tools in order to achieve detailed information about the structure-activity relationships. Following this approach, psoralen derivatives, thought as DNA G-quadruplex stabilizers, were synthesized. For these compounds no biological assays were performed so far. Finally, the last part of the thesis has been dedicated to the synthesis of 1-alkyl-8-(piperazine-1-sulphonyl)phenyl xanthines as high-selective A2B antagonists. Even though the leading role of adenosine and their receptors in cancer pathogenesis were extensively documented, the high therapeutic potential of these compounds requires a wider analysis of their pharmacological properties. Also in this case, several compounds were synthesized. Some of them were tested in a radioligand binding assay to evaluate the affinity and selectivity toward A2BR subtype, further confirming the high potential of these compounds as A2B antagonists."]},{"key":"dc:title","label":"Title","values":["Design and synthesis of new potential anticancer agents and high-selective A2B antagonists"]}]}],"canonical_facts":{"dc:creator":["ARRIDU, ANTONELLA"],"dc:date":["2016-03-24"],"dc:description":["The synthesis of antitumor agents covers a large part of current medicinal chemistry efforts. This thesis mainly focuses on the synthesis of different scaffolds as new potential anticancer agents. Two different approaches were applied: a hybrid concept and a rational based drug design. In the first case, the hybrid concept is useful since it allows combining multiple active scaffolds in a unique molecule. As a consequence, several targets could be hit simultaneously, making this solution particularly attractive for multi-factorial diseases like cancer. Within this category, several isatin-thiazolinone-pyrazoline hybrids were synthesized. Some of them were submitted to biological assays, demonstrating good activity toward different solid tumour cell-lines. In the second class of compounds, the synthetic efforts were combined to computational tools in order to achieve detailed information about the structure-activity relationships. Following this approach, psoralen derivatives, thought as DNA G-quadruplex stabilizers, were synthesized. For these compounds no biological assays were performed so far. Finally, the last part of the thesis has been dedicated to the synthesis of 1-alkyl-8-(piperazine-1-sulphonyl)phenyl xanthines as high-selective A2B antagonists. Even though the leading role of adenosine and their receptors in cancer pathogenesis were extensively documented, the high therapeutic potential of these compounds requires a wider analysis of their pharmacological properties. Also in this case, several compounds were synthesized. Some of them were tested in a radioligand binding assay to evaluate the affinity and selectivity toward A2BR subtype, further confirming the high potential of these compounds as A2B antagonists."],"dc:identifier":["http://hdl.handle.net/11584/266708"],"dc:language":["eng"],"dc:publisher":["Università degli Studi di Cagliari"],"dc:relation":["numberofpages:122"],"dc:rights":["info:eu-repo/semantics/openAccess","license:Non specificato"],"dc:subject":["anticancer","antitumorali","design","progettazione","sintesi","synthesis","Settore CHIM/08 - Chimica Farmaceutica"],"dc:title":["Design and synthesis of new potential anticancer agents and high-selective A2B antagonists"],"dc:type":["info:eu-repo/semantics/doctoralThesis"]},"updated_at":"2026-07-24T01:30:12Z"}