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Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799.

Ohwada J, Ebiike H, Kawada H, Tsukazaki M, Nakamura M, Miyazaki T, Morikami K, Yoshinari K, Yoshida M, Kondoh O, Kuramoto S, Ogawa K, Aoki Y, Shimma N
Bioorg Med Chem Lett 21 1767-72 (2011)
Related entries: 3apc, 3apd

Cited: 34 times
EuropePMC logo PMID: 21316229

Abstract

Phosphatidylinositol 3-kinase (PI3K) is a lipid kinase and a promising therapeutic target for cancer. Using structure-based drug design (SBDD), we have identified novel PI3K inhibitors with a dihydropyrrolopyrimidine skeleton. Metabolic stability of the first lead series was drastically improved by replacing phenol with aminopyrimidine moiety. CH5132799, a novel class I PI3K inhibitor, exhibited a strong inhibitory activity especially against PI3Kα (IC(50)=0.014 μM). In human tumor cell lines with PI3K pathway activation, CH5132799 showed potent antiproliferative activity. CH5132799 is orally available and showed significant antitumor activity in PI3K pathway-activated human cancer xenograft models in mice.

Reviews - 3apf mentioned but not cited (1)

  1. Advances in chemical proteomic evaluation of lipid kinases-DAG kinases as a case study. Ware TB, Hsu KL. Curr Opin Chem Biol 65 101-108 (2021)

Articles - 3apf mentioned but not cited (4)

  1. AMDock: a versatile graphical tool for assisting molecular docking with Autodock Vina and Autodock4. Valdés-Tresanco MS, Valdés-Tresanco ME, Valiente PA, Moreno E. Biol Direct 15 12 (2020)
  2. Formononetin Improves the Survival of Random Skin Flaps Through PI3K/Akt-Mediated Nrf2 Antioxidant Defense System. Li H, Jiang R, Lou L, Jia C, Zou L, Chen M. Front Pharmacol 13 901498 (2022)
  3. "In-silico Design and Development of Novel Hydroxyurea Lipid Drug Conjugates for Breast Cancer Therapy Targeting PI3K/AKT/mTOR Pathway". Dharmaraj S, Swaroop AK, Esakkimuthukumar M, Negi P, Jubie S. Drug Res (Stuttg) 74 32-41 (2024)
  4. Development of New Thiophene-Containing Triaryl Pyrazoline Derivatives as PI3Kγ Inhibitors. Yang B, Zhang B, Zhao Q, Li J, Shi Y. Molecules 27 2404 (2022)


Reviews citing this publication (12)

  1. Application and interpretation of current autophagy inhibitors and activators. Yang YP, Hu LF, Zheng HF, Mao CJ, Hu WD, Xiong KP, Wang F, Liu CF. Acta Pharmacol Sin 34 625-635 (2013)
  2. PI3K-AKT-mTOR inhibition in cancer immunotherapy, redux. O'Donnell JS, Massi D, Teng MWL, Mandala M. Semin Cancer Biol 48 91-103 (2018)
  3. Pharmacologic agents targeting autophagy. Vakifahmetoglu-Norberg H, Xia HG, Yuan J. J Clin Invest 125 5-13 (2015)
  4. Targeting the PI3K signaling pathway in cancer therapy. Bartholomeusz C, Gonzalez-Angulo AM. Expert Opin Ther Targets 16 121-130 (2012)
  5. Recent advances in the use of PI3K inhibitors for glioblastoma multiforme: current preclinical and clinical development. Zhao HF, Wang J, Shao W, Wu CP, Chen ZP, To ST, Li WP. Mol Cancer 16 100 (2017)
  6. PI3K inhibitors are finally coming of age. Vanhaesebroeck B, Perry MWD, Brown JR, André F, Okkenhaug K. Nat Rev Drug Discov 20 741-769 (2021)
  7. PI3K Inhibitors in Cancer: Clinical Implications and Adverse Effects. Mishra R, Patel H, Alanazi S, Kilroy MK, Garrett JT. Int J Mol Sci 22 3464 (2021)
  8. Targeting the unfolded protein response in cancer. Ojha R, Amaravadi RK. Pharmacol Res 120 258-266 (2017)
  9. Wnt and PI3K/Akt/mTOR Survival Pathways as Therapeutic Targets in Glioblastoma. Barzegar Behrooz A, Talaie Z, Jusheghani F, Łos MJ, Klonisch T, Ghavami S. Int J Mol Sci 23 1353 (2022)
  10. Recent syntheses of PI3K/Akt/mTOR signaling pathway inhibitors. Welker ME, Kulik G. Bioorg Med Chem 21 4063-4091 (2013)
  11. Computer-aided targeting of the PI3K/Akt/mTOR pathway: toxicity reduction and therapeutic opportunities. Li T, Wang G. Int J Mol Sci 15 18856-18891 (2014)
  12. Targeting autophagy as a strategy for drug discovery and therapeutic modulation. Gao L, Jauregui CE, Teng Y. Future Med Chem 9 335-345 (2017)

Articles citing this publication (17)

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  12. Optimization of the phenylurea moiety in a phosphoinositide 3-kinase (PI3K) inhibitor to improve water solubility and the PK profile by introducing a solubilizing group and ortho substituents. Kawada H, Ebiike H, Tsukazaki M, Yamamoto S, Koyama K, Nakamura M, Morikami K, Yoshinari K, Yoshida M, Ogawa K, Shimma N, Tsukuda T, Ohwada J. Bioorg Med Chem 24 2897-2906 (2016)
  13. Tumor Growth in the High Frequency Medulloblastoma Mouse Model Ptch1+/-/Tis21KO Has a Specific Activation Signature of the PI3K/AKT/mTOR Pathway and Is Counteracted by the PI3K Inhibitor MEN1611. Ceccarelli M, D'Andrea G, Micheli L, Gentile G, Cavallaro S, Merlino G, Papoff G, Tirone F. Front Oncol 11 692053 (2021)
  14. Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. Wang J, Wang X, Chen Y, Chen S, Chen G, Tong L, Meng L, Xie Y, Ding J, Yang C. Bioorg Med Chem Lett 22 339-342 (2012)
  15. Design, Synthesis and Biological Evaluation of 4-Aryl-5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one Derivatives as a PI3Kα Inhibitor. Hu S, Zhao Z, Ni Y, Xin H, Yan H, Song X. Biol Pharm Bull 42 1013-1018 (2019)
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