Advanced search
Publication Cover
Journal of Enzyme Inhibition and Medicinal Chemistry Volume 34, 2019 - Issue 1
Submit an article Journal homepage
1,518
Views
4
CrossRef citations to date
0
Altmetric
Research Paper

Discovery of aminopyridine-containing spiro derivatives as EGFR mutations inhibitors

Lianbao YeSchool of Pharmacy, Guangdong Pharmaceutical University, Guangzhou, China;
,
Tao ZhaoSchool of Pharmacy, Guangdong Pharmaceutical University, Guangzhou, China;
,
Wenjun DuSchool of Pharmacy, Guangdong Pharmaceutical University, Guangzhou, China;
,
Anhu LiEsa Biotech Co., LTD., Guangzhou, China;
,
Wei GaoSchool of Pharmacy, Guangdong Pharmaceutical University, Guangzhou, China;
,
Jingrong LiEsa Biotech Co., LTD., Guangzhou, China;
,
Ling WangJoint International Research Laboratory of Synthetic Biology and Medicine, Guangdong Provincial Engineering and Technology Research Center of Biopharmaceuticals, School of Biology and Biological Engineering, South China University of Technology, Guangzhou, ChinaORCID Iconhttp://orcid.org/0000-0001-5116-7749
ORCID Icon &
Weiqiang ChenSchool of Basic Courses, Guangdong Pharmaceutical University, Guangzhou, China; Correspondence[email protected]
 show all
Pages 1233-1246 | Received 27 Feb 2019, Accepted 13 Jun 2019, Published online: 09 Jul 2019

References

  • Ciardiello F, Tortora G. A novel approach in the treatment of cancer: targeting the epidermal growth factor receptor. Clin Cancer Res 2001;7:2958–70.
  • Rexer BN, Ghosh R, Narasanna A, et al. Human breast cancer cells harboring a gatekeeper T798M mutation in HER2 overexpress EGFR ligands and are sensitive to dual inhibition of EGFR and HER2. Clin Cancer Res 2013;19:5390–401.
  • Gonzaga IM, Soares-Lima SC, de Santos PT, et al. Alterations in epidermal growth factor receptors 1 and 2 in esophageal squamous cell carcinomas. BMC Cancer 2012;12:569.
  • Johnston S, Leary A. Lapatinib: a novel EGFR/HER2 tyrosine kinase inhibitor for cancer. Drugs Today 2006;42:441–53.
  • Reid A, Vidal L, Shaw H, et al. Dual inhibition of ErbB1 (EGFR/HER1) and ErbB2 (HER2/neu). Eur J Cancer 2007;43:481–9.
  • Ishikawa T, Seto M, Banno H, et al. Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo [3, 2-d] pyrimidine scaffold. J Med Chem 2011;54:8030–50.
  • Doi T, Takiuchi H, Ohtsu A, et al. Phase I first-in-human study of TAK-285, a novel investigational dual HER2/EGFR inhibitor, in cancer patients. Br J Cancer 2012;106:666–72.
  • Assenat E, Azria D, Mollevi C, et al. Dual targeting of HER1/EGFR and HER2 with cetuximab and trastuzumab in patients with metastatic pancreatic cancer after gemcitabine failure： results of the “THERAPY” phase 1-2 trial. Oncotarget 2015;6:12796–808.
  • Tiwari SR, Mishra P, Abraham J. Neratinib, A Novel HER2-targeted tyrosine kinase inhibitor. Clin Breast Cancer 2016;16:344–8.
  • Gandhi L, Bahleda R, Tolaney SM, et al. Phase I study of neratinib in combination with temsirolimus in patients with human epidermal growth factor receptor 2-dependent and other solid tumors. J Clin Oncol 2014;32:68–75.
  • Yun CH, Mengwasser KE, Toms AV, et al. The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP. Proc Natl Acad Sci USA 2008;105:2070–5.
  • Satoshi S, Youichi K, Shigeru I, et al. Structure-based approach for the discovery of Pyrrolo[3,2-d]pyrimidine-Based EGFR T790M/L858R mutant inhibitors. ACS Med Chem Lett 2013;4:201–5.
  • Schwab CL, English DP, Roque DM, et al. Neratinib shows efficacy in the treatment of HER2/neu amplified uterine serous carcinoma in vitro, and in vivo. Gynecol Oncol 2014;135:142–8.
  • Saura C, Garcia-Saenz JA, Xu B, et al. Safety and efficacy of neratinib in combination with capecitabine in patients with metastatic human epidermal growth factor receptor 2epositive breast cancer. J Clin Oncol 2014;32:3626–33.
  • Chan A, Delaloge S, Holmes FA, et al. Neratinib after trastuzumab-based adjuvant therapy in early-stage HER2t breast cancer: a multicentre, randomised, doubleblind, placebo-controlled, phase 3 trial. Lancet Oncol 2016;17:366–77.
  • Ye LB, Tian YX, Li ZH, et al. Design, synthesis and molecular docking studies of some novel spiro[indoline-3, 4′-piperidine]-2-ones as potential c-Met inhibitors. Eur J Med Chem 2012;50:370–5.
  • Balius TE, Rizzo RC. Quantitative prediction of fold resistance for inhibitors of EGFR. Biochemistry 2009;48:8435–48.
  • Aertgeerts K, Skene R, Yano J, et al. Structural analysis of the mechanism of inhibition and allosteric activation of the kinase domain of HER2 protein. J Biol Chem 2011;286:18756–65.
  • Bello M, Saldaña-Rivero L, Correa-Basurto J, etal. Structural and energetic basis for the molecular recognition of dual synthetic vs. natural inhibitors of EGFR/HER2. Int J Biol Macromol 2018;118:1948–62.
  • Bello M, Saldaña-Rivero L, Correa-Basurto J, et al. Binding mechanism of kinase inhibitors to EGFR and T790M, L858R and L858R/T790M mutants through structural and energetic analysis. Int J Biol Macromol 2018;111:569–86.
  • Marawan A, Maiada MS, Khaled AA, et al. In silico design: extended molecular dynamic simulations of a new series of dually acting inhibitors against EGFR and HER2. J Mol Graph Model 2013;44:220–31.
  • Andrea S, György GF, György MK. Comparative evaluation of covalent docking tools. J Chem Inf Model 2018;58:1441–58.

Related research

People also read lists articles that other readers of this article have read.

Recommended articles lists articles that we recommend and is powered by our AI driven recommendation engine.

Cited by lists all citing articles based on Crossref citations.
Articles with the Crossref icon will open in a new tab.