2 research outputs found
Trimeric Hemibastadin Congener from the Marine Sponge <i>Ianthella basta</i>
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>
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)