ArticleJournal of medicinal chemistry2024
Improved Rigidin-Inspired Antiproliferative Agents with Modifications on the 7-Deazahypoxanthine C7/C8 Ring Systems.
Aletta E van der Westhuyzen, Naghmana Ashraf, Daleen Conradie, Leigh Loots, Catherine H Kaschula, Stephen C Pelly, Liliya V Frolova, Taylor Landfair, Charles B Shuster, Tania Betancourt and 2 more
Abstract read
In one paragraphArticle in Journal of medicinal chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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2 · The registryThe trial behind it
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4 · The recordCorrections and comments
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5 · Who and what moneyAuthors and funding
12 authors.
Aletta E van der WesthuyzenDepartment of Chemistry and Polymer Science, Stellenbosch University, Stellenbosch 7600, South Africa.
Naghmana AshrafDepartment of Biology, New Mexico State University, Las Cruces ,New Mexico 88003, United States.
Daleen ConradieDepartment of Chemistry and Polymer Science, Stellenbosch University, Stellenbosch 7600, South Africa.
Leigh LootsDepartment of Chemistry and Polymer Science, Stellenbosch University, Stellenbosch 7600, South Africa.ORCID 0000-0003-3561-5155 Catherine H KaschulaDepartment of Chemistry and Polymer Science, Stellenbosch University, Stellenbosch 7600, South Africa.ORCID 0000-0001-7594-5269 Stephen C PellyDepartment of Chemistry and Polymer Science, Stellenbosch University, Stellenbosch 7600, South Africa.
Liliya V FrolovaDepartment of Chemistry and Biochemistry, Purdue University, 2101 East Coliseum Blvd. ,Fort Wayne ,Indiana 46805, United States.
Taylor LandfairDepartment of Biology, New Mexico State University, Las Cruces ,New Mexico 88003, United States.
Charles B ShusterDepartment of Biology, New Mexico State University, Las Cruces ,New Mexico 88003, United States.
Tania BetancourtDepartment of Chemistry and Biochemistry, Texas State University, San Marcos ,Texas 78666, United States.ORCID 0000-0002-2460-6133 Alexander KornienkoDepartment of Chemistry and Biochemistry, Texas State University, San Marcos ,Texas 78666, United States.ORCID 0000-0003-2041-7367 Willem A L van OtterloDepartment of Chemistry and Polymer Science, Stellenbosch University, Stellenbosch 7600, South Africa.ORCID 0000-0002-3300-6463 Funding
G-RISE at New Mexico State UniversityT32GM148394 · NIGMS · NEW MEXICO STATE UNIVERSITY LAS CRUCES · PI Jessica Perea Houston, Charles Bradley Shuster · 2023 to 2026
$2.1MParameters that determine cell fate during mitotic arrestR16GM145387 · NIGMS · NEW MEXICO STATE UNIVERSITY LAS CRUCES · PI SHUSTER, CHARLES BRADLEY · 2022 to 2025
$676kNIGMS NIH HHS R16 GM145387NIGMS NIH HHS T32 GM148394
6 · The paper itselfAbstract
To improve their aqueous solubility characteristics, water-solubilizing groups were added to some antiproliferative, rigidin-inspired 7-deazahypoxanthine frameworks after molecular modeling seemed to indicate that structural modifications on the C7 and/or C8 phenyl groups would be beneficial. To this end, two sets of 7-deazahypoxanthines were synthesized by way of a multicomponent reaction approach. It was subsequently determined that their antiproliferative activity against HeLa cells was retained for those derivatives with a glycol ether at the 4'-position of the C8 aryl ring system, while also significantly improving their solubility behavior. The best of these compounds were the equipotent 6-[4-(2-ethoxyethoxy)benzoyl]-2-(pent-4-yn-1-yl)-5-phenyl-1,7-dihydro-4
Indexed as
Antineoplastic AgentsCell ProliferationBenzodiazepinesDrug Screening Assays, AntitumorHeLa CellsHumansModels, MolecularSolubilityStructure-Activity RelationshipTubulinAntineoplastic AgentsBenzodiazepinesTubulin
Identifiers
PMID38865195
PMCPMC11215747
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