Výsledky vyhledávání

Aminopyrimidinone Cdc7 Kinase Inhibitors

Autor: Niru B. Soni, Eric F. Johnson, Joel D. Leverson, Thomas D. Penning, Keith W. Woods, Yan Shi, Loren M. Lasko, Julie M. Miyashiro, Alan S. Florjancic, E. K.-H. Han, Chunqiu Lai, Alexander R. Shoemaker, Yunsong Tong

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:1940-1943

We have investigated the SAR of a series of pyrimidinone-containing Cdc7 kinase inhibitors. A wide range of amine substitutions give potent compounds with activities (K(i)) less than 1nM. Kinase selectivity is reasonable and cytotoxicity corresponds

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bdf3f74c76d9ced20f6761e60f152a42
https://doi.org/10.1016/j.bmcl.2012.01.041

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Efficient preparation of S-aryl thioacetates from aryl halides and potassium thioacetate

Autor: Bradley J. Backes, Chunqiu Lai

Publikováno v: Tetrahedron Letters. 48:3033-3037

A method for the preparation of S-aryl thioacetates using palladium-mediated couplings of aryl bromides and aryl triflates with potassium thioacetate as an inexpensive thiol source was developed. Electron withdrawing groups, electron donating groups

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::067b5e2bf27da090c86b5b39e898c07e
https://doi.org/10.1016/j.tetlet.2007.02.128

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Benzoxazole benzenesulfonamides are novel allosteric inhibitors of fructose-1,6-bisphosphatase with a distinct binding mode

Autor: Celerino Abad-Zapatero, Melissa M. Daly, Rebecca J. Gum, Thomas W. von Geldern, Elizabeth H. Fry, Chaohong Sun, Chunqiu Lai

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 16:1811-1815

We have identified benzoxazole benzenesulfonamide 1 as a novel allosteric inhibitor of fructose-1,6-bisphosphatase (FBPase-1). X-ray crystallographic and biological studies of 1 indicate a distinct binding mode that recapitulates features of several

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f318b6eab239d414ab267467a2b71afc
https://doi.org/10.1016/j.bmcl.2006.01.015

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Discovery and structure-activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV inhibitors

Autor: Xiaofeng Li, Thomas W. von Geldern, Kenton L. Longenecker, James M. Trevillyan, Chunqiu Lai, Kent D. Stewart, Bradley J. Backes, Thomas H. Lubben, Daisy Pireh, Anita J Kempf-Grote, Hing L. Sham, Zhonghua Pei, David W A Beno, Stephen J. Ballaron

Publikováno v: Journal of medicinal chemistry. 50(8)

Dipeptidyl peptidase IV (DPP4) inhibitors are emerging as a new class of therapeutic agents for the treatment of type 2 diabetes. They exert their beneficial effects by increasing the levels of active glucagon-like peptide-1 and glucose-dependent ins

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8928389905d050ffae5e4709d0eb7a96
https://pubmed.ncbi.nlm.nih.gov/17367123

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Pyrrolidine-constrained phenethylamines: The design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit

Publikováno v: Bioorganicmedicinal chemistry letters. 17(7)

A novel series of pyrrolidine-constrained phenethylamines were developed as dipeptidyl peptidase IV (DPP4) inhibitors for the treatment of type 2 diabetes. The cyclohexene ring of lead-like screening hit 5 was replaced with a pyrrolidine to enable pa

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f67ad812a62c9eb3983707a663206f0f
https://pubmed.ncbi.nlm.nih.gov/17276063

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Benzoxazole Benzenesulfonamides as Allosteric Inhibitors of Fructose-1,6-bisphosphatase

Autor: Thomas W. von Geldern, Celerino Abad-Zapatero, Melissa M. Daly, Charles W. Hutchins, Elizabeth H. Fry, Chunqiu Lai, Rebecca J. Gum

Publikováno v: ChemInform. 37

A series of novel benzoxazole benzenesulfonamides was synthesized as inhibitors of fructose-1,6-bisphosphatase (FBPase-1). Extensive SAR studies led to a potent inhibitor, 53 , with an IC 50 of 0.57 μM. Compound 17 exhibited excellent bioavailabilit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::434342aed947843bb20ab2f43cff77f4
https://doi.org/10.1002/chin.200627131

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Nonracemic homopropargylic alcohols via asymmetric allenylboration with the robust and versatile 10-TMS-9-borabicyclo[3.3.2]decanes

Autor: John A. Soderquist, Chunqiu Lai

Publikováno v: Organic letters. 7(5)

The asymmetric allenylboration of representative aldehydes with the stable, storable 1 is reported. Easily and efficiently prepared in either enantiomeric form from the air-stable crystalline 4 through simple Grignard procedures, 1 gives 6 cleanly. T

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8576f7b2373dcc45b2852aabb1c3951c
https://pubmed.ncbi.nlm.nih.gov/15727444

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