Zobrazeno 1 - 10
of 21
pro vyhledávání: '"Katerina Otrubova"'
Autor:
Benjamin F. Cravatt, Shreyosree Chatterjee, Dale L. Boger, Srijana Ghimire, Katerina Otrubova
Publikováno v:
Bioorganic & Medicinal Chemistry. 27:1693-1703
A series of N-acyl pyrazoles was examined as candidate serine hydrolase inhibitors in which the active site acylating reactivity and the leaving group ability of the pyrazole could be tuned not only through the nature of the acyl group (reactivity: a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9163729fd60a22e86c6a7617c75bc900
https://doi.org/10.1016/j.bmc.2019.03.020
https://doi.org/10.1016/j.bmc.2019.03.020
Publikováno v:
Tetrahedron. 74:5715-5724
A wide array of synthetic methods are described in the literature for the preparation of xanthones—a prominent class of tricyclic molecules that occur widely in nature. Majority of these reported methods involve linking the two aromatic rings and f
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::cd588c747e7f37566923220e85af37e3
https://doi.org/10.1016/j.tet.2018.08.007
https://doi.org/10.1016/j.tet.2018.08.007
Publikováno v:
Journal of Medicinal Chemistry
A series of α-ketooxazoles incorporating electrophiles at the C5 position of the pyridyl ring of 2 (OL-135) and related compounds were prepared and examined as inhibitors of fatty acid amide hydrolase (FAAH) that additionally target the cytosolic po
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a3fa5d23aad6af1a3ffedc773d91f7e0
http://europepmc.org/articles/PMC3940414
http://europepmc.org/articles/PMC3940414
Publikováno v:
ACS Medicinal Chemistry Letters. 4:985-988
A series of disubstituted C20′-urea derivatives of vinblastine were prepared from 20′-aminovinblastine that was made accessible through a unique Fe(III)/NaBH4-mediated alkene functionalization reaction of anhydrovinblastine. Three analogues were
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cb9ccf0418961f923a4cf03bc2f6dfda
https://doi.org/10.1021/ml400281w
https://doi.org/10.1021/ml400281w
Autor:
Dale L. Boger, Scott T. O'Neal, Raymond C. Stevens, Gye Won Han, Aron H. Lichtman, Katerina Otrubova, Monica Brown, Benjamin F. Cravatt, Michael S. McCormick
Publikováno v:
Journal of the American Chemical Society. 135:6289-6299
The design and characterization of α-ketoheterocycle fatty acid amide hydrolase (FAAH) inhibitors are disclosed that additionally and irreversibly target a cysteine (Cys269) found in the enzyme cytosolic port while maintaining the reversible covalen
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::476fd4bcfe814510f821bfebf7ab48bf
https://doi.org/10.1021/ja4014997
https://doi.org/10.1021/ja4014997
Publikováno v:
Journal of Medicinal Chemistry. 50:1999-2002
We have identified five derivatives of the natural product sansalvamide A that are potent against multiple drug-resistant colon cancer cell lines. These analogs share no structural homology to current colon cancer drugs, are cytotoxic at levels on pa
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::23bffb3aff9814e30bfb109488016c2d
https://doi.org/10.1021/jm070088s
https://doi.org/10.1021/jm070088s
Autor:
Po-Shen Pan, Shelli R. McAlpine, Irene Medina, Ricardo Corral, Emily Parry, Julia Cajica, Chung-Mao Pan, Ahmet Kekec, Thomas J. Styers, Christopher Carroll, Rodrigo A. Rodriguez, Kathleen L. McGuire, Stephanie A. Lapera, Joseph D. Brown, Katerina Otrubova
Publikováno v:
Bioorganic & Medicinal Chemistry. 14:5625-5631
We report the synthesis of thirty-six Sansalvamide A derivatives, and their biological activity against colon cancer HT-29 cell line, a microsatellite stable (MSS) colon cancer cell-line. The thirty-six compounds can be divided into three subsets, wh
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0617201c6be26ac4f77b5c334f2dc832
https://doi.org/10.1016/j.bmc.2006.04.031
https://doi.org/10.1016/j.bmc.2006.04.031
Two libraries of modestly reactive ureas containing either electron-deficient acyl anilines or acyl pyrazoles were prepared and are reported as screening libraries for candidate serine hydrolase inhibitors. Within each library is a small but powerful
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::57962ec79b5422f4de1d7d803d3521ab
https://europepmc.org/articles/PMC4130767/
https://europepmc.org/articles/PMC4130767/
A summary of the discovery and advancement of inhibitors of fatty acid amide hydrolase (FAAH) is presented.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::311975859fad7c2834fb20fd4a4242e4
https://europepmc.org/articles/PMC3146581/
https://europepmc.org/articles/PMC3146581/
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(20)
Key studies leading to the discovery and definition of the role of endogenous fatty acid amide signaling molecules are summarized.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::82a7d5c97bfafa17bb87c6452af1c05d
https://pubmed.ncbi.nlm.nih.gov/20817522
https://pubmed.ncbi.nlm.nih.gov/20817522