Literature DB >> 28835805

Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity.

Chengbin Yang1, Xi Zhang2, Yi Wang2, Yongtai Yang1, Xiaofeng Liu1, Mingli Deng1, Yu Jia1, Yun Ling1, Ling-Hua Meng2, Yaming Zhou1.   

Abstract

The phosphoinositide 3-kinase (PI3K) inhibitors potently inhibit the signaling pathway of PI3K/AKT/mTOR, which provides a promising new approach for the molecularly targeted cancer therapy. In this work, a novel series of 7-azaindole scaffold derivatives was discovered by the fragment-based growing strategy. The structure-activity relationship profiles identified that the 7-azaindole scaffold derivatives exhibit potent activity against PI3K at molecular and cellular levels as well as cell proliferation in a panel of human tumor cells.

Entities:  

Keywords:  1H-pyrrolo[2,3-b] pyridine; PI3K; PI3K/mTOR; cancer therapy; oncology

Year:  2017        PMID： 28835805      PMCID： PMC5554905          DOI： 10.1021/acsmedchemlett.7b00222

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  30 in total

Review 1.  The phosphatidylinositol 3-Kinase AKT pathway in human cancer.

Authors:  Igor Vivanco; Charles L Sawyers
Journal:  Nat Rev Cancer       Date:  2002-07       Impact factor: 60.716

Review 2.  Selective PI3Kδ inhibitors, a review of the patent literature.

Authors:  Peter Norman
Journal:  Expert Opin Ther Pat       Date:  2011-11       Impact factor: 6.674

Review 3.  Molecules in medicine mini-review: isoforms of PI3K in biology and disease.

Authors:  Bart Vanhaesebroeck; Maria A Whitehead; Roberto Piñeiro
Journal:  J Mol Med (Berl)       Date:  2015-12-10       Impact factor: 4.599

Review 4.  PI3K and cancer: lessons, challenges and opportunities.

Authors:  David A Fruman; Christian Rommel
Journal:  Nat Rev Drug Discov       Date:  2014-02       Impact factor: 84.694

Review 5.  PI3K in cancer: divergent roles of isoforms, modes of activation and therapeutic targeting.

Authors:  Lauren M Thorpe; Haluk Yuzugullu; Jean J Zhao
Journal:  Nat Rev Cancer       Date:  2015-01       Impact factor: 60.716

6.  A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma.

Authors:  Qi-Wen Fan; Zachary A Knight; David D Goldenberg; Wei Yu; Keith E Mostov; David Stokoe; Kevan M Shokat; William A Weiss
Journal:  Cancer Cell       Date:  2006-05       Impact factor: 31.743

Review 7.  Targeting the phosphoinositide 3-kinase pathway in cancer.

Authors:  Pixu Liu; Hailing Cheng; Thomas M Roberts; Jean J Zhao
Journal:  Nat Rev Drug Discov       Date:  2009-08       Impact factor: 84.694

8.  The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer .

Authors:  Adrian J Folkes; Khatereh Ahmadi; Wendy K Alderton; Sonia Alix; Stewart J Baker; Gary Box; Irina S Chuckowree; Paul A Clarke; Paul Depledge; Suzanne A Eccles; Lori S Friedman; Angela Hayes; Timothy C Hancox; Arumugam Kugendradas; Letitia Lensun; Pauline Moore; Alan G Olivero; Jodie Pang; Sonal Patel; Giles H Pergl-Wilson; Florence I Raynaud; Anthony Robson; Nahid Saghir; Laurent Salphati; Sukhjit Sohal; Mark H Ultsch; Melanie Valenti; Heidi J A Wallweber; Nan Chi Wan; Christian Wiesmann; Paul Workman; Alexander Zhyvoloup; Marketa J Zvelebil; Stephen J Shuttleworth
Journal:  J Med Chem       Date:  2008-09-25       Impact factor: 7.446

Review 9.  Clinical development of phosphatidylinositol 3-kinase inhibitors for cancer treatment.

Authors:  Irene Brana; Lillian L Siu
Journal:  BMC Med       Date:  2012-12-11       Impact factor: 8.775

Review 10.  Phosphatidylinositol 3-kinase (PI3K) inhibitors as cancer therapeutics.

Authors:  Akintunde Akinleye; Parthu Avvaru; Muhammad Furqan; Yongping Song; Delong Liu
Journal:  J Hematol Oncol       Date:  2013-11-22       Impact factor: 17.388
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  4 in total

1.  Azaindole therapeutic agents.

Authors:  Damoder Reddy Motati; Radhika Amaradhi; Thota Ganesh
Journal:  Bioorg Med Chem       Date:  2020-10-30       Impact factor: 3.641

2.  QSAR analysis on a large and diverse set of potent phosphoinositide 3-kinase gamma (PI3Kγ) inhibitors using MLR and ANN methods.

Authors:  Fereydoun Sadeghi; Abbas Afkhami; Tayyebeh Madrakian; Raouf Ghavami
Journal:  Sci Rep       Date:  2022-04-12       Impact factor: 4.379

3.  A Unique GSK-3β inhibitor B10 Has a Direct Effect on Aβ, Targets Tau and Metal Dyshomeostasis, and Promotes Neuronal Neurite Outgrowth.

Authors:  Xiao-Long Shi; Ning Yan; Ying-Jie Cui; Zhao-Peng Liu
Journal:  Cells       Date:  2020-03-07       Impact factor: 6.600

4.  Design, Synthesis, Biological Evaluation, and Molecular Modeling of 2-Difluoromethylbenzimidazole Derivatives as Potential PI3Kα Inhibitors.

Authors:  Xiangcong Wang; Moxuan Zhang; Ranran Zhu; Zhongshan Wu; Fanhong Wu; Zhonghua Wang; Yanyan Yu
Journal:  Molecules       Date:  2022-01-08       Impact factor: 4.411
  4 in total

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