Pharmacophore identification of c-Myc inhibitor 10074-G5
JL Yap, H Wang, A Hu, J Chauhan, KY Jung…
Index: Yap, Jeremy L.; Wang, Huabo; Hu, Angela; Chauhan, Jay; Jung, Kwan-Young; Gharavi, Robert B.; Prochownik, Edward V.; Fletcher, Steven Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 1 p. 370 - 374
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Citation Number: 24
Abstract
A structure–activity relationship (SAR) study of the c-Myc (Myc) inhibitor 10074-G5 (N-([1, 1′-biphenyl]-2-yl)-7-nitrobenzo [c][1, 2, 5] oxadiazol-4-amine, 1)–which targets a hydrophobic domain of the Myc oncoprotein that is flanked by arginine residues–was executed in order to determine its pharmacophore. Whilst the 7-nitrobenzofurazan was found to be critical for inhibitory activity, the ortho-biphenyl could be replaced with a para- ...
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