Literature DB >> 15006393

Discovery of novel heteroaryl-substituted chalcones as inhibitors of TNF-alpha-induced VCAM-1 expression.

Charles Q Meng1, X Sharon Zheng, Liming Ni, Zhihong Ye, Jacob E Simpson, Kimberly J Worsencroft, Martha R Hotema, M David Weingarten, Jason W Skudlarek, Joshua M Gilmore, Lee K Hoong, Russell R Hill, Elaine M Marino, Ki-Ling Suen, Charles Kunsch, Martin A Wasserman, James A Sikorski.   

Abstract

Novel chalcone derivatives have been discovered as potent inhibitors of TNF-alpha-induced VCAM-1 expression. Thienyl or benzothienyl substitution at the meta-position of ring B helps boost potency while large substitution at the para-position on ring B is detrimental. Various substitutions are tolerated on ring A. A lipophilicity-potency relationship has been observed in several sub-series of compounds.

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Year:  2004        PMID: 15006393     DOI: 10.1016/j.bmcl.2004.01.021

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Artemisia dracunculus L. Ethanolic Extract and an Isolated Component, DMC2, Ameliorate Inflammatory Signaling in Pancreatic β-Cells via Inhibition of p38 MAPK.

Authors:  Peter Smoak; Susan J Burke; Thomas M Martin; Heidi M Batdorf; Z Elizabeth Floyd; J Jason Collier
Journal:  Biomolecules       Date:  2022-05-15

2.  1-Phenyl-3-(2,4,6-trimethoxy-phen-yl)prop-2-en-1-one.

Authors:  Ying Liu; Xianxi Zhang; Zechun Xue; Chunyan Lv
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2009-10-13
  2 in total

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