Natural Product Research · 2018 · 16 citations · 12 references
PharmacyBiochemistryMicrobiologyBioorganic ChemistryDrug DiscoveryStructure-activity RelationshipsEnzyme InhibitionStructure-activity Relationship AnalysisBioactivity ScreeningBromodomain InhibitionBromodomain ProteinsEnzyme Inhibition Screening
One new indolocarbazole alkaloid, 12-N-methyl-k252c, together with eight known indolocarbazoles were isolated from the rice solid fermentation of the marine-derived Streptomyces sp. A22. Their structures were elucidated on the basis of spectroscopic methods (UV, IR, HRESITOF MS, 1D NMR and 2D NMR). All of these compounds were evaluated for bromodomain-containing protein 4 (BRD4) inhibitory activities and cytotoxic activity assay, respectively. Compounds 4 and 5 showed moderate cytotoxic activity with an IC50 value of 3.52 and 3.93 μM, respectively. Additionally, compound 1 also was tested for enzyme inhibition activities of protein kinases and showed moderate activity with IC50 values of 0.91–1.84 μM.
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New Colorimetric Cytotoxicity Assay for Anticancer-Drug Screening
Philip Skehan, Ritsa Storeng, Dominic A. Scudiero et al. · JNCI Journal of the National Cancer Institute · 1990 · 9.8K citations
Medicine, Oncology, Pharmacology +10
Elisabète Rodrigues Pereira, Laure Belin, Martine Sancelme et al. · Journal of Medicinal Chemistry · 1996 · 135 citations · Full text