Browsing by Author "Pelly, Stephen C."

Now showing 1 - 3 of 3
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    Synthesis of 2-substituted tetrahydroisoquinolin-6-ols: potential scaffolds for estrogen receptor modulation and / or microtubule degradation
    (ARKAT USA, 2019) Mabank, Tanya; Alexandre, Kabamba B.; Pelly, Stephen C.; Green, Ivan R.; Van Otterlo, Willem A. L.
    ENGLISH ABSTRACT: 6-Methoxytetrahydroisoquinoline hydrochloride was converted into four small libraries of substituted ureas, thioureas, sulfonamides and N-aryls, using the tetrahydroisoquinoline nitrogen as the scaffold-linking atom. Some of the compounds were evaluated for their ability to inhibit cell proliferation using the MCF7 (invasive ductal carcinoma) cell line.
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    Synthesis of novel piperazine-linked anthranilic acids as potential small molecule kinase inhibitors
    (South African Chemical Institute, 2014-03) Chakravorty, Santanu; Klein, Hanna F.; Hodson, Luke E.; Rabillier, Matthias; Fang, Zhizhou; Richters, Andre; Pelly, Stephen C.; Rauh, Daniel; Van Otterlo, Willem A. L.
    Substituted anthranilic acid and piperazines were used as building blocks to prepare two libraries of compounds, with the aim being that they would exhibit biochemical activity as small molecule kinase inhibitors. The synthesized anthranilamidepiperazine compounds were subsequently tested against a panel of kinases including EGFR, Abl, Akt and Aurora B.
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    Synthesis of pyrrolocarbazoles with N-substituted alkynyl-, alkylcyano- and alkylhydroxyl-groups
    (ARKAT USA, 2020) Van der Westhuyzen, Alet E.; Hadjegeorgiou, Kathy; Green, Ivan R.; Pelly, Stephen C.; Van Otterlo, Willem A. L.
    ENGLISH ABSTRACT: Due to their involvement in almost all stages of cellular life, kinase biomolecular catalysts have been linked to cancer development and, thus, remain attractive drug targets for cancer therapeutics. 6-(3ꞌ-Hydroxypropyl)-, 6-(2ꞌ-hydroxyethyl)-, 6-(2ꞌ-propynyl)- and 6-(3ꞌ-propanenitrile)-pyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones were synthesized as potential small molecule EGFR kinase inhibitors. The pyrrolocarbazole compounds were synthesized by way of a Diels-Alder approach involving N-alkylated 2-vinyl-1H-indole and maleimide as starting materials followed by aromatization with MnO2.