Review of the article „Synthesis and Cytotoxicity Evaluation of Novel Indole Derivatives as Potential Anti-Cancer Agents“, verified by Publons, Web of Science
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A series of bioisosteres of marine indole alkaloids (meridianins) was synthesized and the compounds were tested for their in vitro antiproliferative activity against HCT-116 cell-line. In the design of the targeted analogues, the 2-aminopyrimidine ring of merdianins was replaced with 5-aminopyrazoles, pyrazolo[1,5-a]pyrimidines and pyrazolo[3,4-b]pyridines. The cytotoxic screening of the synthesized compounds revealed that pyrazolo[1,5-a]pyrimidines (compounds 9c and 11a) had the most potent cytotoxic activity with IC50 = 0.31 μM and 0.34 μM respectively. Compounds 9c and 11a were further investigated for their kinase inhibitory potencies toward six kinases (CDK5/p25, CK1ð/ɛ, GSK-3α/β, Dyrk1A, Erk2, and CLK1). The results showed that both compounds were highly potent inhibitors of GSK-3α/β and Erk2 enzymes.
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Medicinal Chemistry, 2018, 1/BMS-MC-2018-301-30Kolekcije
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Mašinski fakultetTY - JOUR AU - Jovanović, Tamara PY - 2018 UR - https://machinery.mas.bg.ac.rs/handle/123456789/6134 AB - A series of bioisosteres of marine indole alkaloids (meridianins) was synthesized and the compounds were tested for their in vitro antiproliferative activity against HCT-116 cell-line. In the design of the targeted analogues, the 2-aminopyrimidine ring of merdianins was replaced with 5-aminopyrazoles, pyrazolo[1,5-a]pyrimidines and pyrazolo[3,4-b]pyridines. The cytotoxic screening of the synthesized compounds revealed that pyrazolo[1,5-a]pyrimidines (compounds 9c and 11a) had the most potent cytotoxic activity with IC50 = 0.31 μM and 0.34 μM respectively. Compounds 9c and 11a were further investigated for their kinase inhibitory potencies toward six kinases (CDK5/p25, CK1ð/ɛ, GSK-3α/β, Dyrk1A, Erk2, and CLK1). The results showed that both compounds were highly potent inhibitors of GSK-3α/β and Erk2 enzymes. T2 - Medicinal Chemistry T1 - Review of the article „Synthesis and Cytotoxicity Evaluation of Novel Indole Derivatives as Potential Anti-Cancer Agents“, verified by Publons, Web of Science EP - 30 SP - 1/BMS-MC-2018-301 UR - https://hdl.handle.net/21.15107/rcub_machinery_6134 ER -
@article{ author = "Jovanović, Tamara", year = "2018", abstract = "A series of bioisosteres of marine indole alkaloids (meridianins) was synthesized and the compounds were tested for their in vitro antiproliferative activity against HCT-116 cell-line. In the design of the targeted analogues, the 2-aminopyrimidine ring of merdianins was replaced with 5-aminopyrazoles, pyrazolo[1,5-a]pyrimidines and pyrazolo[3,4-b]pyridines. The cytotoxic screening of the synthesized compounds revealed that pyrazolo[1,5-a]pyrimidines (compounds 9c and 11a) had the most potent cytotoxic activity with IC50 = 0.31 μM and 0.34 μM respectively. Compounds 9c and 11a were further investigated for their kinase inhibitory potencies toward six kinases (CDK5/p25, CK1ð/ɛ, GSK-3α/β, Dyrk1A, Erk2, and CLK1). The results showed that both compounds were highly potent inhibitors of GSK-3α/β and Erk2 enzymes.", journal = "Medicinal Chemistry", title = "Review of the article „Synthesis and Cytotoxicity Evaluation of Novel Indole Derivatives as Potential Anti-Cancer Agents“, verified by Publons, Web of Science", pages = "30-1/BMS-MC-2018-301", url = "https://hdl.handle.net/21.15107/rcub_machinery_6134" }
Jovanović, T.. (2018). Review of the article „Synthesis and Cytotoxicity Evaluation of Novel Indole Derivatives as Potential Anti-Cancer Agents“, verified by Publons, Web of Science. in Medicinal Chemistry, 1/BMS-MC-2018-301-30. https://hdl.handle.net/21.15107/rcub_machinery_6134
Jovanović T. Review of the article „Synthesis and Cytotoxicity Evaluation of Novel Indole Derivatives as Potential Anti-Cancer Agents“, verified by Publons, Web of Science. in Medicinal Chemistry. 2018;:1/BMS-MC-2018-301-30. https://hdl.handle.net/21.15107/rcub_machinery_6134 .
Jovanović, Tamara, "Review of the article „Synthesis and Cytotoxicity Evaluation of Novel Indole Derivatives as Potential Anti-Cancer Agents“, verified by Publons, Web of Science" in Medicinal Chemistry (2018):1/BMS-MC-2018-301-30, https://hdl.handle.net/21.15107/rcub_machinery_6134 .