84907-81-3Relevant academic research and scientific papers
Design, synthesis and anticancer mechanistic studies of linked azoles
Islam, Md. Amirul,Zhang, Yuqi,Wang, Yao,McAlpine, Shelli R.
, p. 300 - 305 (2015/03/30)
Herein we report the synthesis and biological activity evaluation of 2,4 linked azole-containing molecules. A total of 13 linked thiazole- and oxazole-containing compounds were synthesized in good yields. Cytotoxicity evaluation of those compounds showed
Synthesis of macrocycles that inhibit protein synthesis: Stereochemistry and structural based studies on sanguinamide B derivatives
Pietkiewicz, Adrian L.,Wahyudi, Hendra,McConnell, Jeanette R.,McAlpine, Shelli R.
, p. 6979 - 6982 (2015/02/05)
We report the synthesis of seven new sanguinamide B (SanB) analogues. Substitution of amino acids along the backbone of SanB and testing in HCT-116 colon cancer cell lines identified new biologically active SanB derivatives. These compounds establish a st
Mechanistic studies of sanguinamide B derivatives: A unique inhibitor of eukaryotic ribosomes
Tantisantisom, Worawan,Ramsey, Deborah M.,McAlpine, Shelli R.
supporting information, p. 4638 - 4641 (2013/10/08)
Described are mechanistic studies of two Sanguinamide B (San B) derivatives. These compounds were identified as eukaryotic ribosomal inhibitors. Two biotinylated San B derivatives were synthesized and used to capture protein targets in a pull-down assay.
Discovery of a new class of glucosylceramide synthase inhibitors
Koltun, Elena,Richards, Steven,Chan, Vicky,Nachtigall, Jason,Du, Hongwang,Noson, Kevin,Galan, Adam,Aay, Naing,Hanel, Art,Harrison, Amanda,Zhang, Jeff,Won, Kwang-Ai,Tam, Danny,Qian, Fawn,Wang, Tao,Finn, Patricia,Ogilvie, Kathleen,Rosen, Jon,Mohan, Raju,Larson, Christopher,Lamb, Peter,Nuss, John,Kearney, Patrick
scheme or table, p. 6773 - 6777 (2011/12/05)
A novel series of potent inhibitors of glucosylceramide synthase are described. The optimization of biochemical and cellular potency as well as ADME properties led to compound 23c. Broad tissue distribution was obtained following oral administration to mice. Thus 23c could be another useful tool compound for studying the effects of GCS inhibition in vitro and in vivo.
Synthesis of new oxathiazinane dioxides and their in vitro cancer cell growth inhibitory activity
Borcard, Fran?oise,Baud, Matthias,Bello, Claudia,Dal Bello, Giovanna,Grossi, Francesco,Pronzato, Paolo,Cea, Michele,Nencioni, Alessio,Vogel, Pierre
supporting information; experimental part, p. 5353 - 5356 (2010/11/04)
New oxathiazinane dioxides derived from d- and l-serine have been tested for their in vitro cell growth inhibitory activity toward SKBR3 breast cancer cells. Compound (R)-24 (R′ = BrCH2C6H 4-C6H4CH2) showed a cytotoxicity with IC50 ≈ 10 μM.
A class of novel Schiff's bases: Synthesis, therapeutic action for chronic pain, anti-inflammation and 3D QSAR analysis
Zhou, Yinjian,Zhao, Ming,Wu, Yingting,Li, Chunyu,Wu, Jianhui,Zheng, Meiqing,Peng, Li,Peng, Shiqi
experimental part, p. 2165 - 2172 (2010/05/18)
To discover analgesics for treating chronic pain 17 novel Schiff's bases, N,N′-(Z-allylidene-1,3-diyl)bisamino acid methyl esters were prepared from 1,1,3,3,-tetramethoxypropane and amino acid methyl esters. On tail-flick mouse model 20 μmol/kg of these Schiff's bases were orally administered, the analgesic action started 30 min after administration, reached the maximum 120 min after administration, and at 180 min this action was still observed. On a xylene-induced ear edema mouse model 20 μmol/kg of these Schiff's bases exhibited desirable anti-inflammation. Thus the present Schiff's bases are able to treat chronic pain from inflammation. The effect of the side chains of the amino acid residues of these Schiff's bases on the analgesic activity was explained with 3D QSAR.
NOVEL DIHYDROXYPYRROLIDINE DERIVATIVES AS ANTI-CANCER AGENTS
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Page/Page column 21-22, (2009/10/22)
The present invention provides new dihydroxypyrrolidine derivatives for use as medicaments. The compounds are useful in the treatment in cancer, in particular non-solid neoplasms.
Efficient three-step sequence for the deamination of α-aminoesters. Application to the synthesis of CysLT1 antagonists
González, Alfredo,Pérez, Daniel,Puig, Carles,Ryder, Hamish,Sanahuja, Jordi,Solé, Laia,Bach, Jordi
supporting information; experimental part, p. 2750 - 2753 (2009/09/25)
A practical and efficient three-step sequence for the deamination of α-aminoesters is reported. This method is based on the NaBH4-mediated selective reduction of α-diazoesters to α-hydrazonoesters and has been successfully applied to the deamin
A microwave enhanced cross-metathesis approach to peptidomimetics
Morris, Thomas,Sandham, David,Caddick, Stephen
, p. 1025 - 1027 (2008/01/01)
Functionalization of amino acid C- and N-termini with appropriate olefinic moieties allows for the generation of a peptidomimetic via a stereoselective cross-metathesis. This journal is The Royal Society of Chemistry.
PIPERAZINE UREA DERIVATIVES FOR THE TREATMENT OF ENDOMETRIOSIS
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Page/Page column 92, (2008/06/13)
Use of a compound of the following formula (Ia) for the production of a medicament for the treatment of endometriosis in human wherein the treatment comprises administering to a human female in need of such treatment a therapeutically effective amount of said compound.
