English (United Kingdom)

https://curated-unify.zendy.io/wp-json/zendy-region/v1/featured_content/oa?rat=en

https://curated-unify.zendy.io/wp-json/zendy-region/v1/highlighted_journal/

Global: Zendy Plus annual

Presents the access of premium content as premium feature

Premium Content

Presents the keyphrase highlighting as premium feature

Keyphrase Highlighting

Presents the summarisation as premium feature

Summarisation

Insights

Presents the pdf analysis as premium feature

PDF Analysis

Presents the zaia usage as premium feature

ZAIA

Global: Zendy Tools annual

Global: Zendy Free Plan

Global: Zendy Tools monthly

Global: Zendy Plus monthly

Three new aaptamines ( 1–3 ) together with two known derivatives ( 4–5 ) were isolated from the South China Sea sponge  Aaptos suberitoides . The structures of all compounds were unambiguously elucidated by spectroscopic analyses as well as the comparison with literature data. All the compounds were evaluated for their cytotoxic activities against five human cancer cell lines including H1299, H520, SCG7901, CNE-2 and SW680 cells. As a result, compounds  3–5  showed moderate cytotoxicities against H1299 and H520 cells with IC 50  values ranging from 12.9 to 20.6 μg/mL. Besides, compounds  3–5  also showed potent inhibitory activities toward cyclin-dependent kinase-2 (CDK2) with IC 50  values of 14.3, 3.0 and 6.0 μg/mL, respectively. In addition, compounds  3–5  significantly induced G1 arrests of H1299 cells at low concentrations. Drug affinity responsive target stability (DARTS) experiments were carried out and further demonstrated that compound  3  could effectively bind with CDK2 protein and protect it from the degradation by pronase.

Aaptamine derivatives with CDK2 inhibitory activities from the South China Sea sponge Aaptos suberitoides