329190-48-9Relevant academic research and scientific papers
Mediators of hedgehog signaling pathways, compositions and uses related thereto
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Page/Page column 69; 70; 71; 72, (2015/11/27)
The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function by contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize hedgehog activity.
Potent inhibitors of the Hedgehog signaling pathway
Brunton, Shirley A.,Stibbard, John H. A.,Rubin, Lee L.,Kruse, Lawrence I.,Guicherit, Oivin M.,Boyd, Edward A.,Price, Steven
, p. 1108 - 1110 (2008/09/19)
A small family of phenyl quinazolinone ureas is reported as potent modulators of Hedgehog protein function. Preliminary SAR studies of the urea substituent led to a nanomolar Hedgehog antagonist.
Synthesis and structure-activity relationships of vasicine analogues as bronchodilatory agents
Mahindroo, Neeraj,Ahmed, Zabeer,Bhagat, Asha,Bedi, Kasturi Lal,Khajuria, Ravi Kant,Kapoor, Vijay Kumar,Dhar, Kanaya Lal
, p. 347 - 368 (2007/10/03)
The series of vasicine (1) analogues, an alkaloid from Adhatoda vasica Nees., were synthesized with changes in A, B or C rings. Compounds 3-19 were evaluated for in vitro bronchodilatory activity using isolated guinea pig tracheal chain. Compounds 3-8 were also synthesized in good yields using microwave-mediated synthesis under solvent free conditions. Compounds 5 and 8 with seven-member C ring were more active than etofylline and caused 100% relaxation of both the histamine and acetylcholine pre-contracted guinea pig tracheal chain. The structure-activity relationship studies showed that the quinazoline and oxo functionalities were essential for activity. The compounds without C ring and instead having aliphatic and phenyl substitutions in B ring showed relaxation against histamine pre-contracted tracheal chain only, 2-methyl substituted analogues, 12 and 13, being most active with 100% relaxation effect. Birkhaeuser Boston 2006.
Synthesis and structure-activity relationship of 3-phenyl-3H-quinazolin-4- one derivatives as CXCR3 chemokine receptor antagonists
Storelli, Stefania,Verdijk, Pauline,Verzijl, Dennis,Timmerman, Henk,Van De Stolpe, Andrea C.,Tensen, Cornelis P.,Smit, Martine J.,De Esch, Iwan J. P.,Leurs, Rob
, p. 2910 - 2913 (2007/10/03)
A series of 3-phenyl-3H-quinazolin-4-ones have been synthesized and tested for affinity and activity at the chemokine CXCR3 receptor. The most potent compound (1d) has been evaluated using radioligand binding and calcium mobilization assays and is considered a useful tool for further characterization of the CXCR3 receptor.
Mediators of hedgehog signaling pathways, compositions and uses related thereto
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, (2008/06/13)
The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function by contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growt
Compounds and methods for modulating cxcr3 function
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, (2008/06/13)
The invention provides compounds and compositions of the formula: wherein the subscript n is an integer of from 0 to 4; Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl; Rs
CXCR3 antagonists
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, (2008/06/13)
Compounds, compositions and methods that are useful in the treatment of inflammatory and immune conditions and diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of a chemokine receptor. The subject methods are useful for the treatment of inflammatory and immunoregulatory disorders and diseases, such as multiple sclerosis, rheumatoid arthritis and type I diabetes.
