2 research outputs found

    Trimeric Hemibastadin Congener from the Marine Sponge <i>Ianthella basta</i>

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    The first naturally occurring trimeric hemibastadin congener, sesquibastadin 1 (<b>1</b>), and the previously reported bastadins 3, 6, 7, 11, and 16 (<b>2</b>–<b>6</b>) were isolated from the marine sponge <i>Ianthella basta</i>, collected in Indonesia. The structure of <b>1</b> was elucidated on the basis of 1D and 2D NMR measurements and by HRMS. Among all the isolated compounds, the linear sesquibastadin 1 (<b>1</b>) and bastadin 3 (<b>2</b>) showed the strongest inhibition rates for at least 22 protein kinases (IC<sub>50</sub> = 0.1–6.5 μM), while the macrocyclic bastadins (<b>3</b>–<b>6</b>) demonstrated a strong cytotoxic potential against the murine lymphoma cell line L5178Y (IC<sub>50</sub> = 1.5–5.3 μM)

    Cytotoxic and Protein Kinase Inhibiting Nakijiquinones and Nakijiquinols from the Sponge <i>Dactylospongia metachromia</i>

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    Chemical investigation of the sponge <i>Dactylospongia metachromia</i> afforded five new sesquiterpene aminoquinones (<b>1</b>–<b>5</b>), two new sesquiterpene benzoxazoles (<b>6</b> and <b>7</b>), the known analogue 18-hydroxy-5-<i>epi</i>-hyrtiophenol (<b>8</b>), and a known glycerolipid. The structures of all compounds were unambiguously elucidated by one- and two-dimensional NMR and by MS analyses, as well as by comparison with the literature. Compounds <b>1</b>–<b>5</b> showed potent cytotoxicity against the mouse lymphoma cell line L5178Y with IC<sub>50</sub> values ranging from 1.1 to 3.7 μM. When tested <i>in vitro</i> for their inhibitory potential against 16 different protein kinases, compounds <b>5</b>, <b>6</b>, and <b>8</b> exhibited the strongest inhibitory activity against ALK, FAK, IGF1-R, SRC, VEGF-R2, Aurora-B, MET wt, and NEK6 kinases (IC<sub>50</sub> 0.97–8.62 μM)
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