Development of antiproliferative phenylmaleimides that activate the unfolded protein response

…, T Kosakowska-Cholody, D Farnsworth, M Dyba…

Index: Muus, Ulrike; Hose, Curtis; Yao, Wei; Kosakowska-Cholody, Teresa; Farnsworth, David; Dyba, Marzena; Lountos, George T.; Waugh, David S.; Monks, Anne; Burke Jr., Terrence R.; Michejda, Christopher J. Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 12 p. 4535 - 4541

Full Text: HTML

Citation Number: 7

Abstract

The current paper presents the synthesis and evaluation of a series of maleimides that were designed to inhibit the Cdc25 phosphatase by alkylation of catalytically essential cysteine residues. Although in HepB3 cell culture assays the analogues did exhibit antiproliferative IC50 values ranging from sub-micromolar to greater than 100μM, inhibition of Cdc25 through cysteine alkylation could not be demonstrated. It was also found that analysis ...

Related Articles:

Synthesis of substituted bis (heteroaryl) maleimides

[Dubernet, Mathieu; Caubert, Virginie; Guillard, Jerome; Viaud-Massuard, Marie-Claude Tetrahedron, 2005 , vol. 61, # 19 p. 4585 - 4593]

A mild synthesis of N-functionalised bromomaleimides, thiomaleimides and bromopyridazinediones

[Castaneda, Lourdes; Wright, Zoe V.F.; Marculescu, Cristina; Tran, Trang M.; Chudasama, Vijay; Maruani, Antoine; Hull, Elizabeth A.; Nunes, Joao P.M.; Fitzmaurice, Richard J.; Smith, Mark E.B.; Jones, Lyn H.; Caddick, Stephen; Baker, James R. Tetrahedron Letters, 2013 , vol. 54, # 27 p. 3493 - 3495]

Revised structures of N-substituted dibrominated pyrrole derivatives and their polymeric products. Termaleimide models with low optical band gaps

[Choi, Dong-Sook; Huang, Shenlin; Huang, Mingsheng; Barnard, Thomas S.; Adams, Richard D.; Seminario, Jorge M.; Tour, James M. Journal of Organic Chemistry, 1998 , vol. 63, # 8 p. 2646 - 2655]

Revised structures of N-substituted dibrominated pyrrole derivatives and their polymeric products. Termaleimide models with low optical band gaps

[Choi, Dong-Sook; Huang, Shenlin; Huang, Mingsheng; Barnard, Thomas S.; Adams, Richard D.; Seminario, Jorge M.; Tour, James M. Journal of Organic Chemistry, 1998 , vol. 63, # 8 p. 2646 - 2655]

Revised structures of N-substituted dibrominated pyrrole derivatives and their polymeric products. Termaleimide models with low optical band gaps

[Choi, Dong-Sook; Huang, Shenlin; Huang, Mingsheng; Barnard, Thomas S.; Adams, Richard D.; Seminario, Jorge M.; Tour, James M. Journal of Organic Chemistry, 1998 , vol. 63, # 8 p. 2646 - 2655]

More Articles...