3-Thiomorpholin-8-oxo-8H-acenaphtho [1,2-b] pyrrole-9-carbonitrile (S1) derivatives as pan-Bcl-2-inhibitors of Bcl-2, Bcl-xL and Mcl-1

Bioorganic and Medicinal Chemistry

Volumn 21, Issue 1, 2013, Pages 11-20

  Song, Ting ^a   Li, Xiangqian ^a   Chang, Xilong ^b,c   Liang, Xiaomeng ^a   Zhao, Yan ^a   Wu, Guiye ^a   Xie, Shenghui ^a   Su, Pengchen ^a   Wu, Zhiyong ^a   Feng, Yingang ^d   Zhang, Zhichao ^a  

^a DALIAN UNIVERSITY OF TECHNOLOGY   (China)

^b PEKING UNIVERSITY   (China)

^c Qilu Pharmaceutical Co Ltd   (China)

^d QINGDAO INSTITUTE OF BIOENERGY AND BIOPROCESS TECHNOLOGY   (China)

Author keywords

Apoptosis; Bcl 2; Mcl 1; p4 Pocket; Pan Bcl 2 inhibitor

Indexed keywords

3 THIOMORPHOLIN 8 OXO 8H ACENAPHTHO[1,2 B]PYRROLE 9 CARBONITRILE DERIVATIVE; PROTEIN BCL 2; PROTEIN BCL XL; PROTEIN INHIBITOR; PROTEIN MCL 1; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; BINDING SITE; CONTROLLED STUDY; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SOLUBILITY; DRUG STRUCTURE; DRUG TARGETING; ENZYME LINKED IMMUNOSORBENT ASSAY; LIGAND BINDING; NUCLEAR MAGNETIC RESONANCE; SITE DIRECTED MUTAGENESIS; STRUCTURE ACTIVITY RELATION;

ACENAPHTHENES; ANTINEOPLASTIC AGENTS; APOPTOSIS; BCL-X PROTEIN; CELL LINE, TUMOR; DRUG SCREENING ASSAYS, ANTITUMOR; HUMANS; MODELS, MOLECULAR; NEOPLASMS; NITRILES; PROTEIN BINDING; PROTO-ONCOGENE PROTEINS C-BCL-2; PYRROLES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84870952287     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2012.11.008     Document Type: Article

References (24)

1. D.L. Sackett, and D. Sept Nat. Chem. 1 2009 596
2. A.V. Veselovsky, and A.I. Archakov Curr. Comput. Aided Drug Des. 3 2007 51
3. A.S. Azmi, and R.M. Mohammad J. Cell. Physiol. 218 2009 13
4. L. Zhang, L. Ming, and J. Yu Drug Resist. Updates 10 2007 207
5. M. Vogler, D. Dinsdale, M.J. Dyer, and G.M. Cohen Cell Death Differ. 16 2009 360
6. M.R. Warr, and G.C. Shore Curr. Mol. Med. 8 2008 138
7. J. Bednarek, J.D. Wesierska, and Z.M. Kilianska Postepy Biochem. 53 2007 228
8. M.F.V. Delft, A.H. Wei, K.D. Mason, C.J. Vandenberg, L. Chen, P.E. Czabotar, S.N. Willis, C.L. Scott, C.L. Day, S. Cory, J.M. Adams, A.W. Roberts, and D.C. Huang Cancer Cell 10 2006 389
9. M. Konopleva, R. Contractor, T. Tsao, I. Samudio, P.P. Ruvolo, S. Kitada, X. Deng, D. Zhai, Y.X. Shi, and T. Sneed Cancer Cell 10 2006 375
10. Z.C. Zhang, L.J. Jin, X.H. Qian, M.J. Wei, Y.Y. Wang, and J. Wang ChemBioChem 8 2007 113
11. Z.C. Zhang, T. Song, T.T. Zhang, J. Gao, G.Y. Wu, and L.J. An Int. J. Cancer 128 2010 1724
12. Z.C. Zhang, G.Y. Wu, F.B. Xie, T. Song, and X.L. Chang J. Med. Chem. 54 2011 1101
13. E.F. Lee, P.E. Czabotar, B.J. Smith, K. Deshayes, K. Zobel, P.M. Colman, and W.D. Fairlie Cell Death Differ. 14 2007 1711
14. G. Wang, Z. Nikolovska-Coleska, C.Y. Yang, R. Wang, G. Tang, J. Guo, S. Shanqary, S. Qiu, W. Gao, and D. Yang J. Med. Chem. 49 2006 6139
15. S. Acoca, Q. Cui, G.C. Shore, and E.O. Purisima Proteins 79 2011 2624
16. P.E. Czabotar, E.F. Lee, M.F. Van Delft, C. Day, B.J. Smith, and D.C.S. Huang Proc. Natl. Acad. Sci. U.S.A. 104 2007 6217
17. M. Bruncko, T.K. Oost, B.A. Belli, H. Ding, M.K. Joseph, A. Kunzer, D. Martineau, W.J. McClellan, M. Mitten, and S.C. Nq J. Med. Chem. 50 2007 641
18. G. Tang, Z. Nikolovska-Coleska, S. Qiu, C.Y. Yang, J. Guo, and S. Wang J. Med. Chem. 51 2008 717
19. E. Fire, S.V. Gulla, R.A. Grant, and A.E. Keating Protein Sci. 19 2010 507
20. P. Ballard, R.H. Bradbury, C.S. Harris, L.F. Hennequin, M. Hickinson, J.G. Kettle, J. Kendrew, T. Klinowska, D.J. Ogilvie, S.E. Pearson, E.J. Williams, and I. Wilson Bioorg. Med. Chem. Lett. 16 2006 4908
21. S. Lopes, L. Lapinski, and R. Fausto Phys. Chem. Chem. Phys. 4 2002 5952
22. E.F. Lee, P.E. Czabotar, M.F. Delft, E.M. Michalak, M.J. Boyle, S.N. Willis, H. Puthalakath, P. Bouillet, P.M. Colman, D.C. Huang, and W.D. Fairlie J. Cell Biol. 180 2008 341
23. E.J. Mui, G.A. Schiehser, W.K. Milhous, H. Hsu, C.W. Roberts, M. Kirisits, S. Muench, D. Rice, J.P. Dubey, and J.W. Fowble PLoS Negl. Trop. Dis. 2 2008 e190
24. X. Lei, Y. Chen, G. Du, W. Yu, X. Wang, H. Qu, B. Xia, H. He, J. Mao, and W. Zong FASEB J. 20 2006 2147