Literature DB >> 22386982

Perturbing pro-survival proteins using quinoxaline derivatives: a structure-activity relationship study.

Rajkumar Rajule1, Vashti C Bryant, Hernando Lopez, Xu Luo, Amarnath Natarajan.   

Abstract

In HeLa cells the combinatorial knockdown of Bcl-xL and Mcl-1 is sufficient to induce spontaneous apoptosis. Quinoxaline derivatives were screened for the induction of Mcl-1 dependent apoptosis using a cell line without functional Bcl-xL. Quinoxaline urea analog 1 h was able to specifically induce apoptosis in an Mcl-1 dependent manner. We demonstrate that even small changes to 1h results in dramatic loss of activity. In addition, 1 h and ABT-737 synergistically inhibit cell growth and induce apoptosis. Our results also suggest that 1h could have therapeutic potential against ABT-737 refractory cancer.
Copyright © 2012 Elsevier Ltd. All rights reserved.

Entities:  

Mesh：

Substances：

Year:  2012        PMID： 22386982      PMCID： PMC3303926          DOI： 10.1016/j.bmc.2012.02.022

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  50 in total

1.  QUINACILLIN: A COMPARISON WITH OTHER PENICILLINASE-RESISTANT PENICILLINS.

Authors:  J T SMITH; J M HAMILTON-MILLER; R KNOX
Journal:  Nature       Date:  1964-09-12       Impact factor: 49.962

Review 2.  Recent developments in bisintercalator natural products.

Authors:  Olga E Zolova; Ahmed S A Mady; Sylvie Garneau-Tsodikova
Journal:  Biopolymers       Date:  2010-09       Impact factor: 2.505

3.  Synthesis and biological activities of pyrazolo[3,4-g]quinoxaline derivatives.

Authors:  Laurent Gavara; Emmanuelle Saugues; Georges Alves; Eric Debiton; Fabrice Anizon; Pascale Moreau
Journal:  Eur J Med Chem       Date:  2010-09-15       Impact factor: 6.514

4.  Influence of Bcl-2 family members on the cellular response of small-cell lung cancer cell lines to ABT-737.

Authors:  Stephen K Tahir; Xiufen Yang; Mark G Anderson; Susan E Morgan-Lappe; Aparna V Sarthy; Jun Chen; Robert B Warner; Shi-Chung Ng; Stephen W Fesik; Steve W Elmore; Saul H Rosenberg; Christin Tse
Journal:  Cancer Res       Date:  2007-02-01       Impact factor: 12.701

Review 5.  IAPs: more than just inhibitors of apoptosis proteins.

Authors:  Laurence Dubrez-Daloz; Alban Dupoux; Jessy Cartier
Journal:  Cell Cycle       Date:  2008-02-11       Impact factor: 4.534

6.  BMS-345541 is a highly selective inhibitor of I kappa B kinase that binds at an allosteric site of the enzyme and blocks NF-kappa B-dependent transcription in mice.

Authors:  James R Burke; Mark A Pattoli; Kurt R Gregor; Patrick J Brassil; John F MacMaster; Kim W McIntyre; Xiaoxia Yang; Violetta S Iotzova; Wendy Clarke; Joann Strnad; Yuping Qiu; F Christopher Zusi
Journal:  J Biol Chem       Date:  2002-10-25       Impact factor: 5.157

Review 7.  Cleavage of poly(ADP-ribose) polymerase: a sensitive parameter to study cell death.

Authors:  P J Duriez; G M Shah
Journal:  Biochem Cell Biol       Date:  1997       Impact factor: 3.626

8.  Inhibition of bcl-2 enhances the efficacy of chemotherapy in renal cell carcinoma.

Authors:  I Kausch; H Jiang; B Thode; C Doehn; S Krüger; D Jocham
Journal:  Eur Urol       Date:  2005-01-15       Impact factor: 20.096

Review 9.  Mechanisms of caspase activation and inhibition during apoptosis.

Authors:  Yigong Shi
Journal:  Mol Cell       Date:  2002-03       Impact factor: 17.970

10.  Cdc25B dual-specificity phosphatase inhibitors identified in a high-throughput screen of the NIH compound library.

Authors:  Paul A Johnston; Caleb A Foster; Marni Brisson Tierno; Tong Ying Shun; Sunita N Shinde; William D Paquette; Kay M Brummond; Peter Wipf; John S Lazo
Journal:  Assay Drug Dev Technol       Date:  2009-06       Impact factor: 1.738
View more
  17 in total

1.  A quinoxaline urea analog uncouples inflammatory and pro-survival functions of IKKβ.

Authors:  Dulce Maroni; Sandeep Rana; Chandrani Mukhopadhyay; Amarnath Natarajan; Mayumi Naramura
Journal:  Immunol Lett       Date:  2015-10-27       Impact factor: 3.685

2.  Targeting the NF-κB and mTOR pathways with a quinoxaline urea analog that inhibits IKKβ for pancreas cancer therapy.

Authors:  Prakash Radhakrishnan; Vashti C Bryant; Elizabeth C Blowers; Rajkumar N Rajule; Nagsen Gautam; Muhammad M Anwar; Ashley M Mohr; Paul M Grandgenett; Stephanie K Bunt; Jamie L Arnst; Subodh M Lele; Yazen Alnouti; Michael A Hollingsworth; Amarnath Natarajan
Journal:  Clin Cancer Res       Date:  2013-02-26       Impact factor: 12.531

3.  Novel treatment for mantle cell lymphoma including therapy-resistant tumor by NF-κB and mTOR dual-targeting approach.

Authors:  Nagendra K Chaturvedi; Rajkumar N Rajule; Ashima Shukla; Prakash Radhakrishnan; Gordon L Todd; Amarnath Natarajan; Julie M Vose; Shantaram S Joshi
Journal:  Mol Cancer Ther       Date:  2013-08-20       Impact factor: 6.261

4.  Chemical Genetic Screens Identify Kinase Inhibitor Combinations that Target Anti-Apoptotic Proteins for Cancer Therapy.

Authors:  Jacob I Contreras; Caroline M Robb; Hannah M King; Jared Baxter; Ayrianne J Crawford; Smit Kour; Smitha Kizhake; Yogesh A Sonawane; Sandeep Rana; Michael A Hollingsworth; Xu Luo; Amarnath Natarajan
Journal:  ACS Chem Biol       Date:  2018-04-05       Impact factor: 5.100

5.  Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy.

Authors:  Sandeep Rana; Yogesh A Sonawane; Margaret A Taylor; Smitha Kizhake; Muhammad Zahid; Amarnath Natarajan
Journal:  Bioorg Med Chem Lett       Date:  2018-10-15       Impact factor: 2.823

6.  In Vitro and In Vivo Activities of 2,3-Diarylsubstituted Quinoxaline Derivatives against Leishmania amazonensis.

Authors:  Vanessa Kaplum; Juliana Cogo; Diego Pereira Sangi; Tânia Ueda-Nakamura; Arlene Gonçalves Corrêa; Celso Vataru Nakamura
Journal:  Antimicrob Agents Chemother       Date:  2016-05-23       Impact factor: 5.191

7.  Isatin Derived Spirocyclic Analogues with α-Methylene-γ-butyrolactone as Anticancer Agents: A Structure-Activity Relationship Study.

Authors:  Sandeep Rana; Elizabeth C Blowers; Calvin Tebbe; Jacob I Contreras; Prakash Radhakrishnan; Smitha Kizhake; Tian Zhou; Rajkumar N Rajule; Jamie L Arnst; Adnan R Munkarah; Ramandeep Rattan; Amarnath Natarajan
Journal:  J Med Chem       Date:  2016-04-26       Impact factor: 7.446

8.  Small molecule binding to inhibitor of nuclear factor kappa-B kinase subunit beta in an ATP non-competitive manner.

Authors:  John V Napoleon; Sarbjit Singh; Sandeep Rana; Mourad Bendjennat; Vikas Kumar; Smitha Kizhake; Nicholas Y Palermo; Michel M Ouellette; Tom Huxford; Amarnath Natarajan
Journal:  Chem Commun (Camb)       Date:  2021-05-11       Impact factor: 6.222

9.  Aminopyrazole based CDK9 PROTAC sensitizes pancreatic cancer cells to venetoclax.

Authors:  Hannah M King; Sandeep Rana; Sydney P Kubica; Jayapal Reddy Mallareddy; Smitha Kizhake; Edward L Ezell; Muhammad Zahid; Michael J Naldrett; Sophie Alvarez; Henry C-H Law; Nicholas T Woods; Amarnath Natarajan
Journal:  Bioorg Med Chem Lett       Date:  2021-04-23       Impact factor: 2.940

10.  Structure activity relationship (SAR) study identifies a quinoxaline urea analog that modulates IKKβ phosphorylation for pancreatic cancer therapy.

Authors:  Satish Sagar; Sarbjit Singh; Jayapal Reddy Mallareddy; Yogesh A Sonawane; John V Napoleon; Sandeep Rana; Jacob I Contreras; Christabelle Rajesh; Edward L Ezell; Smitha Kizhake; Jered C Garrison; Prakash Radhakrishnan; Amarnath Natarajan
Journal:  Eur J Med Chem       Date:  2021-05-30       Impact factor: 7.088
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.