ArticleJournal of medicinal chemistry2020
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
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Article in Journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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Who cites it
30 citing papers in PubMed.
- Design, Synthesis, and Biological Evaluation of Novel Triazine-Based Dual Histone Deacetylase/phosphatidylinositol 3-kinase Inhibitors for Breast Cancer Therapy.ChemMedChem · 2026Article
- DNA Binding, DNA Photocleavage, Molecular Docking Studies and Photo-Induced Effect on Melanoma Cells of 2-Methyl-3-OR Quinazolinone Derivatives.Biomolecules · 2026Article
- Chidamide and Anlotinib act synergistically in Jurkat cells by inhibiting the Hippo signaling pathway.Biochemistry and biophysics reports · 2026Article
- Phosphatidylinositol-3-Kinase (PI3K) and Histone Deacetylase (HDAC) Multitarget Inhibitors: An Update on Clinical and Preclinical Candidates.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Recent progress in the exploitation of anti-cancer small molecules targeting angiogenesis.Journal of enzyme inhibition and medicinal chemistry · 2025Review
- The current status of quinazoline hybrids with antibreast cancer therapeutic potential-part II.Future medicinal chemistry · 2025Review
- The antibreast cancer therapeutic potential of quinazoline hybrids-Part I.Future medicinal chemistry · 2025Review
- Recent Advancements in the Development of HDAC/Tubulin Dual-Targeting Inhibitors.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Structural Modifications and Prospects of Histone Deacetylase (HDAC) Inhibitors in Cancer.Current medicinal chemistry · 2025Review
- Green Synthetic and Pharmacological Developments in the Hybrid Quinazolinone Moiety: An Updated Review.Current topics in medicinal chemistry · 2025Review
- Discovery of novel and potent dual-targeting AXL/HDAC2 inhibitors for colorectal cancer treatment via structure-based pharmacophore modelling, virtual screening, and molecular docking, molecular dynamics simulation studies, and biological evaluation.Journal of enzyme inhibition and medicinal chemistry · 2024Article
- Novel dual-targeting inhibitors of NSD2 and HDAC2 for the treatment of liver cancer: structure-based virtual screening, molecular dynamics simulation, andJournal of enzyme inhibition and medicinal chemistry · 2024Article
- The Histone Deacetylase Family: Structural Features and Application of Combined Computational Methods.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Discovery and Development of HDAC Inhibitors: Approaches for the Treatment of Cancer a Mini-review.Current drug discovery technologies · 2024Review
- Insight in Quinazoline-based HDAC Inhibitors as Anti-cancer Agents.Mini reviews in medicinal chemistry · 2024Review
- Quatramer™ encapsulation of dual-targeted PI3-Kδ/HDAC6 inhibitor, HSB-510, suppresses growth of breast cancer.Bioengineering & translational medicine · 2023Article
- Three-dimensional quantitative structural-activity relationship and molecular dynamics study of multivariate substituted 4-oxyquinazoline HDAC6 inhibitors.Molecular diversity · 2023Article
- Evaluation of the anti-proliferative activity of 2-oxo-pyridine and 1'RSC advances · 2023Article
- Synthesis, Molecular Docking, In Vitro and In Vivo Studies of Novel Dimorpholinoquinazoline-Based Potential Inhibitors of PI3K/Akt/mTOR Pathway.International journal of molecular sciences · 2022Article
- The Intricate Epigenetic and Transcriptional Alterations in Pediatric High-Grade Gliomas: Targeting the Crosstalk as the Oncogenic Achilles' Heel.Biomedicines · 2022Review
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Authors and funding
15 authors.
Ashish ThakurNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.ORCID 0000-0002-8456-1088
Gregory J TawaNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Mark J HendersonNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.ORCID 0000-0001-8590-7338
Carina DanchikNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Suiyang LiuDana-Farber Cancer Institute, 450 Brookline Avenue, Boston, Massachusetts 02215, United States.
Pranav ShahNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Amy Q WangNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Garrett DunnNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Md KabirNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Elias C PadilhaNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Xin XuNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Anton SimeonovNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Surender KharbandaDana-Farber Cancer Institute, 450 Brookline Avenue, Boston, Massachusetts 02215, United States.
Richard StoneDana-Farber Cancer Institute, 450 Brookline Avenue, Boston, Massachusetts 02215, United States.
Gurmit GrewalNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Funding
Pharmacokinetics and Drug MetabolismZIATR000369 · NCATS · NATIONAL CENTER FOR ADVANCING TRANSLATIONAL SCIENCES · PI XU, XIN · 2018 to 2025
$27.3MTRAINING PROGRAM IN CANCER THERAPYT32CA078207 · NCI · MOUNT SINAI SCHOOL OF MEDICINE OF NYU · PI James J Manfredi · 1999 to 2026
$11.6MHDAC/PI3K Dual Inhibitors for Treatment of Rare CancersZIATR000371 · NCATS · NATIONAL CENTER FOR ADVANCING TRANSLATIONAL SCIENCES · PI LO, DONALD · 2018 to 2022
$3.3MIntramural NIH HHS Z99 TR999999NCI NIH HHS T32 CA078207
Abstract
A series of quinazolin-4-one based hydroxamic acids was rationally designed and synthesized as novel dual PI3K/HDAC inhibitors by incorporating an HDAC pharmacophore into a PI3K inhibitor (Idelalisib) via an optimized linker. Several of these dual inhibitors were highly potent (IC
Indexed as
Drug DesignAnimalsCell Line, TumorDrug Evaluation, PreclinicalFemaleHEK293 CellsHistone Deacetylase InhibitorsHumansHydroxamic AcidsMiceMice, Inbred BALB CPhosphatidylinositol 3-KinasesPhosphoinositide-3 Kinase InhibitorsProtein Structure, TertiaryQuinazolinonesRats4-hydroxyquinazolineHistone Deacetylase InhibitorsHydroxamic AcidsPhosphatidylinositol 3-KinasesPhosphoinositide-3 Kinase InhibitorsQuinazolinones
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.