Structural Optimization and MD Simulation Study of Benzimidazole Derivatives as Potent Mutant FLT3 Kinase Inhibitors Targeting AML
Sign Up to like & getrecommendations! Published in 2025 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.70002
Abstract: Acute myeloid leukemia (AML) is an aggressive hematological malignancy with poor survival rates in adults, posing a significant economic burden. FMS‐like tyrosine kinase 3 (FLT3) mutations are linked to poor prognosis in AML and resistance… read more here.
Keywords: potent mutant; mutant flt3; flt3; cell ... See more keywords
α‐Triazolylboronic Acids: A Novel Scaffold to Target FLT3 in AML
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DOI: 10.1002/cmdc.202400622
Abstract: The treatment of acute myeloid leukemia (AML) presents a challenge to current therapies because of the development of drug resistance. Genetic mutation of FMS‐like tyrosine kinase‐3 (FLT3) is a target of interest for AML treatment,… read more here.
Keywords: triazolylboronic acids; flt3; aml; acids novel ... See more keywords
Upfront intensive treatment analysis of the Italian Cohort Study on FLT3‐mutated AML patients (FLAM): The impact of a FLT3 inhibitor addition to standard chemotherapy in the real‐life setting
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DOI: 10.1002/cncr.35824
Abstract: The addition of a FLT3 inhibitor (FLT3i) to standard chemotherapy to treat fit newly diagnosed (ND) patients with FLT3‐mutated acute myeloid leukemia (AML) represents the standard of care resulting from clinical trial results. However, evidence… read more here.
Keywords: standard chemotherapy; flt3; addition; flt3 mutated ... See more keywords
Internal tandem duplication mutations in the tyrosine kinase domain of FLT3 display a higher oncogenic potential than the activation loop D835Y mutation
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DOI: 10.1007/s00277-018-3245-5
Abstract: Acute myeloid leukemia (AML) remains the most common form of acute leukemia among adults and accounts for a large number of leukemia-related deaths. Mutations in FMS-like tyrosine kinase 3 (FLT3) is one of the most… read more here.
Keywords: kinase domain; flt3; domain; tyrosine kinase ... See more keywords
Pre-transplant FLT3/ITD status predicts outcome in FLT3-mutated acute myeloid leukemia following allogeneic stem cell transplantation
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DOI: 10.1007/s00277-020-04026-1
Abstract: Acute myeloid leukemia (AML) with fetal liver tyrosine kinase 3 (FLT3) internal tandem duplication (ITD) is associated with poor prognosis, and allogeneic stem cell transplantation (Allo-SCT) seems to be the preferred therapeutic approach. However, the… read more here.
Keywords: flt3; transplant; flt3 mrd; transplantation ... See more keywords
Preclinical activity and a pilot phase I study of pacritinib, an oral JAK2/FLT3 inhibitor, and chemotherapy in FLT3-ITD-positive AML
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DOI: 10.1007/s10637-019-00786-4
Abstract: SummaryActivating FLT3 internal tandem duplication (FLT3-ITD) mutations in acute myeloid leukemia (AML) associate with inferior outcomes. We determined that pacritinib, a JAK2/FLT3 inhibitor, has in vitro activity against FLT3-ITD and tyrosine kinase domain (TKD) mutations.… read more here.
Keywords: chemotherapy; inhibitor; flt3; cohort ... See more keywords
Significance of FLT3-tyrosine kinase domain mutation as a prognostic factor for acute myeloid leukemia
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DOI: 10.1007/s12185-019-02720-z
Abstract: The prognostic significance of FLT3-tyrosine kinase domain (TKD) mutations remains unknown. To investigate the prognostic impact of FLT3-TKD, 676 de novo acute myeloid leukemia (AML), we retrospectively analyzed cases and conducted a review of the… read more here.
Keywords: positive cases; flt3; significance flt3; flt3 tkd ... See more keywords
Combined inhibition of PI3Kδ and FLT3 signaling exerts synergistic antitumor activity and overcomes acquired drug resistance in FLT3-activated acute myeloid leukemia.
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DOI: 10.1016/j.canlet.2018.01.071
Abstract: PI3Kδ and FLT3 are frequently activated in acute myeloid leukemia (AML) and have been implicated as potential therapeutic targets. In this report, we demonstrate that combined inhibition of PI3Kδ and FLT3 exerts synergistic antitumor activity… read more here.
Keywords: flt3 activated; pi3k flt3; combined inhibition; flt3 ... See more keywords
Discovery of 4-piperazinyl-2-aminopyrimidine derivatives as dual inhibitors of JAK2 and FLT3.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.111590
Abstract: Hybridization strategy is an effective strategy to obtain multi-target inhibitors in drug design. In this study, we assembled the pharmacophores of momelotinib and tandutinib to get a series of 4-piperazinyl-2-aminopyrimidine derivatives. All compounds were tested… read more here.
Keywords: piperazinyl aminopyrimidine; aminopyrimidine derivatives; jak2 flt3; flt3 ... See more keywords
Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases.
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DOI: 10.1016/j.ejmech.2019.111710
Abstract: Aberrant activation of FMS-like tyrosine receptor kinase 3 (FLT3) is implicated in the pathogenesis of acute myeloid leukemia (AML) in 20-30% of patients. In this study we identified a highly selective (phenylethenyl)quinazoline compound family as… read more here.
Keywords: development extreme; discovery development; flt3; extreme selective ... See more keywords
Discovery of novel 4-azaaryl-N-phenylpyrimidin-2-amine derivatives as potent and selective FLT3 inhibitors for acute myeloid leukaemia with FLT3 mutations.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.113215
Abstract: Feline McDonough sarcoma (FMS)-like tyrosine kinase 3 (FLT3) is one of the most pursued targets in the treatment of acute myeloid leukaemia (AML) as its gene amplification and mutations, particularly internal tandem duplication (ITD), contribute… read more here.
Keywords: flt3; myeloid leukaemia; azaaryl phenylpyrimidin; acute myeloid ... See more keywords