Design, synthesis and evaluation of novel 2-thiophen-5-yl-3H-quinazolin-4-one analogues as inhibitors of transcription factors NF-кB and AP-1 mediated …

…, J Williams, D Rogers, KK Vasu, V Sudarsanam

Index: Giri, Rajan S.; Thaker, Hardik M.; Giordano, Tony; Williams, Jill; Rogers, Donna; Vasu, Kamala K.; Sudarsanam, Vasudevan Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 7 p. 2796 - 2808

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Citation Number: 33

Abstract

In an attempt to discover novel inhibitors of NF-κB and AP-1 mediated transcriptional activation utilizing the concept of chemical lead based medicinal chemistry and bioisosterism a series of 2-(2, 3-disubstituted-thiophen-5-yl)-3H-quinazolin-4-one analogs was designed. A facile and simple route for the synthesis of the designed molecules was developed. Synthesized molecules were evaluated for their activity as inhibitors towards ...