135902-07-7Relevant academic research and scientific papers
SUGAR-ANALOG PHOSPHORUS-CONTAINING HETEROCYCLES HAVING AN ANTI-METASTATIC ACTIVITY
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Paragraph 0133; 0134; 0135, (2016/03/04)
The use of compounds of formula (1) as defined in the description, for reducing or preventing the onset of metastases in a patient suffering from cancer. Pharmaceutical compositions for using in human or veterinary medicine, including at least one compoun
C-glycoside mimetics inhibit glioma stem cell proliferation, migration, and invasion
Clarion, Ludovic,Jacquard, Carine,Sainte-Catherine, Odile,Decoux, Marc,Loiseau, Séverine,Rolland, Marc,Lecouvey, Marc,Hugnot, Jean-Philippe,Volle, Jean-No?l,Virieux, David,Pirat, Jean-Luc,Bakalara, Norbert
supporting information, p. 8293 - 8306 (2014/12/11)
This paper reports the design and synthesis of C-glycoside mimetics (d-glycero-d-talo- and d-glycero-d-galactopyranose analogues), a subset of the recently published phostines, belonging to the [1,2]oxaphosphinane core. Eighteen new compounds were tested against 11 cancer cell types belonging to six categories of tumor tissues and three different species. The hit compound 5.3d inhibited invasion and migration of both GBM stem cells (Gli7 and Gli4) and GBM cancer cell lines (C6, SNB75) on fibronectin, vitronectin, and laminin. Ki values for Gli7 and Gli4 migration inhibition on fibronectin were16 and 31 nM respectively. Ki values for invasion inhibition in a 3D system were 46 nM for Gli7 and 290 nM for Gli4. These activities were associated with an antiproliferative effect on Gli4 (EC50 = 5.20 μM) and Gli7 (EC50 = 2.33 μM). In conclusion, the heptopyranose mimetic 5.3d, devoid of toxicity on astrocyte and cortical neuron cultures at concentrations below 100 μM, opens new therapeutic perspectives against glioblastoma.
Renin Inhibitory Pentols Showing Improved Enteral Bioavailability
Kleemann, Heinz-Werner,Heitsch, Holger,Henning, Rainer,Kramer, Werner,Kocher, Walter,et al.
, p. 559 - 567 (2007/10/02)
Incorporation of a C-terminal pentahydroxy functionality led to potent, low molecular weight hydrophilic renin inhibitors lacking the P1' side chain.As these compounds are easy to synthesize and have sufficient water solubility, they were chosen for further study.Compound 33 was transported across rabbit intestinal brush border membrane vesicles and yielded a hypotensive effect in sodium-depleted rhesus monkeys which lasted for 90 min when dosed at 2 mg/kg id.
