Literature DB >> 22608961

Identification of a phenylacylsulfonamide series of dual Bcl-2/Bcl-xL antagonists.

Heidi L Perez1, Patrizia Banfi, Jay Bertrand, Zhen-Wei Cai, James W Grebinski, Kyoung Kim, Jonathan Lippy, Michele Modugno, Joseph Naglich, Robert J Schmidt, Andrew Tebben, Paola Vianello, Donna D Wei, Liping Zhang, Arturo Galvani, Louis J Lombardo, Robert M Borzilleri.   

Abstract

A series of phenylacylsulfonamides has been prepared as antagonists of Bcl-2/Bcl-xL. In addition to potent binding affinities for both Bcl-2 and Bcl-xL, these compounds were shown to induce classical markers of apoptosis in isolated mitochondria. Overall weak cellular potency was improved by the incorporation of polar functionality resulting in compounds with moderate antiproliferative activity.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID： 22608961     DOI： 10.1016/j.bmcl.2012.04.103

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


  6 in total

1.  Cell death and the mitochondria: therapeutic targeting of the BCL-2 family-driven pathway.

Authors:  M J Roy; A Vom; P E Czabotar; G Lessene
Journal:  Br J Pharmacol       Date:  2014-04       Impact factor: 8.739

Review 2.  Small molecules, big targets: drug discovery faces the protein-protein interaction challenge.

Authors:  Duncan E Scott; Andrew R Bayly; Chris Abell; John Skidmore
Journal:  Nat Rev Drug Discov       Date:  2016-04-11       Impact factor: 84.694

3.  Selectivity by small-molecule inhibitors of protein interactions can be driven by protein surface fluctuations.

Authors:  David K Johnson; John Karanicolas
Journal:  PLoS Comput Biol       Date:  2015-02-23       Impact factor: 4.475

4.  Ryanodine receptors are targeted by anti-apoptotic Bcl-XL involving its BH4 domain and Lys87 from its BH3 domain.

Authors:  Tim Vervliet; Irma Lemmens; Elien Vandermarliere; Elke Decrock; Hristina Ivanova; Giovanni Monaco; Vincenzo Sorrentino; Nael Nadif Kasri; Ludwig Missiaen; Lennart Martens; Humbert De Smedt; Luc Leybaert; Jan B Parys; Jan Tavernier; Geert Bultynck
Journal:  Sci Rep       Date:  2015-04-15       Impact factor: 4.379

5.  Structures of BCL-2 in complex with venetoclax reveal the molecular basis of resistance mutations.

Authors:  Richard W Birkinshaw; Jia-Nan Gong; Cindy S Luo; Daisy Lio; Christine A White; Mary Ann Anderson; Piers Blombery; Guillaume Lessene; Ian J Majewski; Rachel Thijssen; Andrew W Roberts; David C S Huang; Peter M Colman; Peter E Czabotar
Journal:  Nat Commun       Date:  2019-06-03       Impact factor: 14.919

6.  Novel [(N-alkyl-3-indolylmethylene)hydrazono]oxindoles arrest cell cycle and induce cell apoptosis by inhibiting CDK2 and Bcl-2: synthesis, biological evaluation and in silico studies.

Authors:  Tarfah Al-Warhi; Mahmoud F Abo-Ashour; Hadia Almahli; Ohoud J Alotaibi; Mohammad M Al-Sanea; Ghada H Al-Ansary; Hanaa Y Ahmed; Mahmoud M Elaasser; Wagdy M Eldehna; Hatem A Abdel-Aziz
Journal:  J Enzyme Inhib Med Chem       Date:  2020-12       Impact factor: 5.051
  6 in total

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