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Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kδ inhibitors.

Qin LY, Ruan Z, Cherney RJ, Dhar TGM, Neels J, Weigelt CA, Sack JS, Srivastava AS, Cornelius LAM, Tino JA, Stefanski K, Gu X, Xie J, Susulic V, Yang X, Yarde-Chinn M, Skala S, Bosnius R, Goldstein C, Davies P, Ruepp S, Salter-Cid L, Bhide RS, Poss MA
Bioorg Med Chem Lett 27 855-861 (2017)
Cited: 10 times
EuropePMC logo PMID: 28108251

Abstract

As demonstrated in preclinical animal models, the disruption of PI3Kδ expression or its activity leads to a decrease in inflammatory and immune responses. Therefore, inhibition of PI3Kδ may provide an alternative treatment for autoimmune diseases, such as RA, SLE, and respiratory ailments. Herein, we disclose the identification of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent, selective and orally bioavailable PI3Kδ inhibitors. The lead compound demonstrated efficacy in an in vivo mouse KLH model.

Reviews - 5ubt mentioned but not cited (2)

  1. Structural Determinants of Isoform Selectivity in PI3K Inhibitors. Miller MS, Thompson PE, Gabelli SB. Biomolecules 9 E82 (2019)
  2. 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 - 5ubt mentioned but not cited (2)

  1. Structural Features that Distinguish Inactive and Active PI3K Lipid Kinases. Zhang M, Jang H, Nussinov R. J Mol Biol 432 5849-5859 (2020)
  2. Study on the Mechanism of Üstikuddus Sherbiti in Ischemic Cerebrovascular Diseases: Based on Network Pharmacology. Gul A, Aimaiti M, Tuerxun T, Amat R, Reheman A, Zhang MF, Memtily N. Evid Based Complement Alternat Med 2022 5581864 (2022)


Reviews citing this publication (2)

  1. Pyrrolo[2,1-f][1,2,4]triazine: a promising fused heterocycle to target kinases in cancer therapy. Singh S, Utreja D, Kumar V. Med Chem Res 31 1-25 (2022)
  2. 4-Aminopyrazolopyrimidine scaffold and its deformation in the design of tyrosine and serine/threonine kinase inhibitors in medicinal chemistry. Chen X, Huang Y, Xu W, Cai Y, Yang Y. RSC Med Chem 13 1008-1028 (2022)

Articles citing this publication (4)

  1. Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors. Hoegenauer K, Soldermann N, Zécri F, Strang RS, Graveleau N, Wolf RM, Cooke NG, Smith AB, Hollingworth GJ, Blanz J, Gutmann S, Rummel G, Littlewood-Evans A, Burkhart C. ACS Med Chem Lett 8 975-980 (2017)
  2. Structural basis for ligand reception by anaplastic lymphoma kinase. Li T, Stayrook SE, Tsutsui Y, Zhang J, Wang Y, Li H, Proffitt A, Krimmer SG, Ahmed M, Belliveau O, Walker IX, Mudumbi KC, Suzuki Y, Lax I, Alvarado D, Lemmon MA, Schlessinger J, Klein DE. Nature 600 148-152 (2021)
  3. Identification of highly potent and selective PI3Kδ inhibitors. Marcoux D, Qin LY, Ruan Z, Shi Q, Ruan Q, Weigelt C, Qiu H, Schieven G, Hynes J, Bhide R, Poss M, Tino J. Bioorg Med Chem Lett 27 2849-2853 (2017)
  4. Carbon dots enhance extracellular matrix secretion for dentin-pulp complex regeneration through PI3K/Akt/mTOR pathway-mediated activation of autophagy. Liu L, Li X, Bu W, Jin N, Meng Y, Wang Y, Wang D, Xu X, Zhou D, Sun H. Mater Today Bio 16 100344 (2022)


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