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Tubulin-based antimitotic mechanism of E7974, a novel analogue of the marine sponge natural product hemiasterlin
TLDR
It is shown that E7974, such as parental hemiasterlin, acts via a tubulin-based antimitotic mechanism, and seems to share a unique, predominantly α-tubulin–targeted mechanism with other hemiasterslin-based compounds, suggesting that, unlike manytubulin-targeted natural products and related drugs, the hemiastlins evolved to mainly target α- Tubulin, not β-tub insulin subunits.
Optimization of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists.
We previously described a series of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepine CCK-A agonists exemplified by compound 1 (GW 5823), which is the first reported binding selective CCK-A full agonist
Antiproliferative compounds of Artabotrys madagascariensis from the Madagascar rainforest
TLDR
Two of the isolates, melodor inol and acetylmelodorinol, were found to display antiproliferative activity against five different tumour cell lines with IC50 values ranging from 2.4 to 12 µM.
Bioconjugation by native chemical tagging of C-H bonds.
TLDR
A general C-H functionalization method for the tagging of natural products and pharmaceuticals using an azide-containing sulfinate reagent that allows the appendage of azidoalkyl chains onto heteroaromatics to be attached to a monoclonal antibody by a "click" reaction.
Serum thymidine kinase 1 activity as a pharmacodynamic marker of cyclin-dependent kinase 4/6 inhibition in patients with early-stage breast cancer receiving neoadjuvant palbociclib
TLDR
Serum TK1 activity is a promising pharmacodynamic marker of palbociclib in ER+ breast cancer, and its value in predicting response to CDK4/6 inhibitors warrants further investigation.
Isolation and synthesis of antiproliferative eupolauridine alkaloids of Ambavia gerrardii from the Madagascar Dry Forest.
Investigation of the Madagascan endemic plant Ambavia gerrardii for antiproliferative activity against the A2780 ovarian cancer cell line led to the isolation of the three new alkaloids
Antiproliferative limonoids of a Malleastrum sp. from the Madagascar rainforest.
Bioassay-guided fractionation of an ethanol extract of a Malleastrum sp. afforded three new limonoids, malleastrones A-C ( 1- 3), respectively. Each limonoid contained a rare tetranortriterpenoid
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