6633-95-0Relevant academic research and scientific papers
NITROGEN RING LINKED DEOXYURIDINE TRIPHOSPHATASE INHIBITORS
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Paragraph 0628, (2018/06/12)
Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.
6-MEMBERED URACIL ISOSTERES
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Paragraph 0717, (2018/06/12)
Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.
HYDANTOIN CONTAINING DEOXYURIDINE TRIPHOSPHATASE INHIBITORS
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Paragraph 0733, (2018/06/12)
Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.
HYDANTOIN CONTAINING DEOXYURIDINE TRIPHOSPHATASE INHIBITORS
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Paragraph 0726, (2018/06/12)
Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.
URACIL CONTAINING COMPOUNDS
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Paragraph 0692, (2018/07/31)
Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.
BROMODOMAIN TARGETING DEGRONIMERS FOR TARGET PROTEIN DEGRADATION
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Page/Page column 491, (2017/12/05)
This invention provides a Degronimer that has an E3 Ubiquitin Ligase targeting moiety (Degron) that can be linked to a Targeting Ligand for a bromodomain protein selected for in vivo degradation to achieve a therapeutic effect, and methods of use and compositions thereof as well as methods for their preparation.
HYDANTOIN CONTAINING DEOXYURIDINE TRIPHOSPHATASE INHIBITORS
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Paragraph 0644, (2017/01/26)
Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.
Nicotinamide phosphoribosyltransferase inhibitors, design, preparation, and structure-activity relationship
Christensen, Mette K.,Erichsen, Kamille D.,Olesen, Uffe H.,Tj?rnelund, Jette,Fristrup, Peter,Thougaard, Annemette,Nielsen, S?ren Jensby,Sehested, Maxwell,Jensen, Peter B.,Loza, Einars,Kalvinsh, Ivars,Garten, Antje,Kiess, Wieland,Bj?rkling, Fredrik
, p. 9071 - 9088 (2014/01/06)
Existing pharmacological inhibitors for nicotinamide phosphoribosyltransferase (NAMPT) are promising therapeutics for treating cancer. By using medicinal and computational chemistry methods, the structure-activity relationship for novel classes of NAMPT inhibitors is described, and the compounds are optimized. Compounds are designed inspired by the NAMPT inhibitor APO866 and cyanoguanidine inhibitor scaffolds. In comparison with recently published derivatives, the new analogues exhibit an equally potent antiproliferative activity in vitro and comparable activity in vivo. The best performing compounds from these series showed subnanomolar antiproliferative activity toward a series of cancer cell lines (compound 15: IC50 0.025 and 0.33 nM, in A2780 (ovarian carcinoma) and MCF-7 (breast), respectively) and potent antitumor in vivo activity in well-tolerated doses in a xenograft model. In an A2780 xenograft mouse model with large tumors (500 mm3), compound 15 reduced the tumor volume to one-fifth of the starting volume at a dose of 3 mg/kg administered ip, bid, days 1-9. Thus, compounds found in this study compared favorably with compounds already in the clinic and warrant further investigation as promising lead molecules for the inhibition of NAMPT.
