Rationally designed multitarget anticancer agents.

No abstract is available for this paper.

• Publication year

  2013

• Venue

  Current Medicinal Chemistry

• Publication date

  2013-03-31

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.2174/0929867311320130009PMID 23410168
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases.

  2012cited by this paper
• Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors.

  2012cited by this paper
• Quinazoline derivatives as potential anticancer agents: a patent review (2007 – 2010)

  2012cited by this paper
• Potent and selective small molecule inhibitors of specific isoforms of Cdc2-like kinases (Clk) and dual specificity tyrosine-phosphorylation-regulated kinases (Dyrk).

  2011cited by this paper
• Molecular targets of phytochemicals for cancer prevention

  2011cited by this paper
• ZRF4, a combi-molecule with increased efficacy as compared with the individual components in chronic lymphocytic leukemia lymphocytes in vitro

  2011cited by this paper
• Quinoline as a privileged scaffold in cancer drug discovery.

  2011cited by this paper
• Synthesis and docking study of 2-phenylaminopyrimidine Abl tyrosine kinase inhibitors.

  2011cited by this paper
• Designed multiple ligands for cancer therapy.

  2011cited by this paper
• Characterization of the potency of epidermal growth factor (EGFR)-DNA targeting combi-molecules containing a hydrolabile carbamate at the 3-position of the triazene chain

  2011cited by this paper
• The combi-targeting concept: mechanism of action of the pleiotropic combi-molecule RB24 and discovery of a novel cell signaling-based combination principle.

  2011cited by this paper
• A bioanalytical investigation on the exquisitely strong in vitro potency of the EGFR-DNA targeting type II combi-molecule ZR2003 and its mitigated in vivo antitumour activity.

  2011cited by this paper
• Utilizing targeted cancer therapeutic agents in combination: novel approaches and urgent requirements

  2010cited by this paper
• A new class of naphthalimide-based antitumor agents that inhibit topoisomerase II and induce lysosomal membrane permeabilization and apoptosis.

  2010cited by this paper
• 5-Deoxykaempferol Plays a Potential Therapeutic Role by Targeting Multiple Signaling Pathways in Skin Cancer

  2010cited by this paper
• The Combi-Targeting Concept: Selective Targeting of the Epidermal Growth Factor Receptor- and Her2-Expressing Cancer Cells by the Complex Combi-Molecule RB24

  2010cited by this paper
• Curcumin―The Paradigm of a Multi-Target Natural Compound with Applications in Cancer Prevention and Treatment

  2010cited by this paper
• Quinazoline-urea, new protein kinase inhibitors in treatment of prostate cancer

  2010cited by this paper
• CUDC-101, a multitargeted inhibitor of histone deacetylase, epidermal growth factor receptor, and human epidermal growth factor receptor 2, exerts potent anticancer activity.

  2010cited by this paper
• Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.

  2010cited by this paper
• Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.

  2010cited by this paper
• Chimeric tyrosine kinase-HDAC inhibitors as antiproliferative agents

  2010cited by this paper
• Anti-angiogenic tyrosine kinase inhibitors: what is their mechanism of action?

  2009cited by this paper
• Synthesis of quinazolines as tyrosine kinase inhibitors.

  2009cited by this paper
• Evaluation of substituted 6-arylquinazolin-4-amines as potent and selective inhibitors of cdc2-like kinases (Clk).

  2009cited by this paper
• Substituted 2-arylbenzothiazoles as kinase inhibitors: hit-to-lead optimization.

  2009cited by this paper
• Design and synthesis of new stabilized combi-triazenes for targeting solid tumors expressing the epidermal growth factor receptor (EGFR) or its closest homologue HER2.

  2009cited by this paper
• Rational Design of Multitargeted Tyrosine Kinase Inhibitors: A Novel Approach

  2009cited by this paper
• Designing multiple ligands - medicinal chemistry strategies and challenges.

  2009cited by this paper
• Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases.

  2009cited by this paper
• Promise and challenges in drug discovery and development of hybrid anticancer drugs

  2009cited by this paper
• Targeting tumors using estrogen receptor ligand conjugates.

  2009cited by this paper
• Interaction of ionizing radiation and ZRBA1, a mixed EGFR/DNA-targeting molecule

  2009cited by this paper
• N-substituted 2'-(aminoaryl)benzothiazoles as kinase inhibitors: hit identification and scaffold hopping.

  2009cited by this paper
• Overview of naphthalimide analogs as anticancer agents.

  2009cited by this paper
• Novel 9-oxo-thiazolo[5,4-f]quinazoline-2-carbonitrile derivatives as dual cyclin-dependent kinase 1 (CDK1)/glycogen synthase kinase-3 (GSK-3) inhibitors: synthesis, biological evaluation and molecular modeling studies.

  2008cited by this paper
• Network pharmacology: the next paradigm in drug discovery.

  2008cited by this paper
• Combi-targeting concept: an optimized single-molecule dual-targeting model for the treatment of chronic myelogenous leukemia

  2008cited by this paper
• Discovery of multitarget inhibitors by combining molecular docking with common pharmacophore matching.

  2008cited by this paper
• Lysosomal membrane permeabilization in cell death

  2008cited by this paper
• Anti-cancer agent siramesine is a lysosomotropic detergent that induces cytoprotective autophagosome accumulation

  2008cited by this paper
• Type II combi-molecules: design and binary targeting properties of the novel triazolinium-containing molecules JDD36 and JDE05

  2007cited by this paper
• Acridine and acridone derivatives, anticancer properties and synthetic methods: where are we now?

  2007cited by this paper
• 2,2,2-Trichloro-N-({2-[2-(dimethylamino)ethyl]-1,3-dioxo-2,3-dihydro-1H-benzo[de]isoquinolin- 5-yl}carbamoyl)acetamide (UNBS3157), a novel nonhematotoxic naphthalimide derivative with potent antitumor activity.

  2007cited by this paper
• Novel nitrogen mustard-armed combi-molecules for the selective targeting of epidermal growth factor receptor overexperessing solid tumors: discovery of an unusual structure-activity relationship.

  2007cited by this paper
• Optimization of novel combi-molecules: identification of balanced and mixed bcr-abl/DNA targeting properties.

  2007cited by this paper
• Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.

  2007cited by this paper
• The Combi-Targeting Concept: In vitro and In vivo Fragmentation of a Stable Combi-Nitrosourea Engineered to Interact with the Epidermal Growth Factor Receptor while Remaining DNA Reactive

  2007cited by this paper
• Molecular hybridization: a useful tool in the design of new drug prototypes.

  2007cited by this paper
• Vincristine induces dramatic lysosomal changes and sensitizes cancer cells to lysosome-destabilizing siramesine.

  2007cited by this paper
• Multi-target therapeutics: when the whole is greater than the sum of the parts.

  2007cited by this paper
• Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2.

  2007cited by this paper
• Can we rationally design promiscuous drugs?

  2006cited by this paper
• The physicochemical challenges of designing multiple ligands.

  2006cited by this paper
• Strategies for optimizing combinations of molecularly targeted anticancer agents

  2006cited by this paper
• Synergistic Antitumor Activity of ZD6474, An Inhibitor of Vascular Endothelial Growth Factor Receptor and Epidermal Growth Factor Receptor Signaling, with Gemcitabine and Ionizing Radiation against Pancreatic Cancer

  2006cited by this paper
• Thiazolo[5,4-f]quinazolin-9-ones, inhibitors of glycogen synthase kinase-3.

  2006cited by this paper
• Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias.

  2006cited by this paper
• The combi-targeting concept: synthesis of stable nitrosoureas designed to inhibit the epidermal growth factor receptor (EGFR).

  2006cited by this paper
• Multitarget-directed drug design strategy: a novel molecule designed to block epidermal growth factor receptor (EGFR) and to exert proapoptotic effects.

  2006cited by this paper
• Synthesis and biological evaluation of new asymmetrical bisintercalators as potential antitumor drugs.

  2006cited by this paper
• The combi-targeting concept: evidence for the formation of a novel inhibitor in vivo

  2006cited by this paper
• Valproic acid, a histone deacetylase inhibitor, enhances sensitivity to doxorubicin in anaplastic thyroid cancer cells.

  2006cited by this paper
• Activity of SU11248, a multitargeted inhibitor of vascular endothelial growth factor receptor and platelet-derived growth factor receptor, in patients with metastatic renal cell carcinoma.

  2006cited by this paper
• Engineering 3-alkyltriazenes to block bcr-abl kinase: a novel strategy for the therapy of advanced bcr-abl expressing leukemias.

  2005cited by this paper
• 3D-QSAR studies on c-Src kinase inhibitors and docking analyses of a potent dual kinase inhibitor of c-Src and c-Abl kinases.

  2005cited by this paper
• Synthesis of half-mustard combi-molecules with fluorescence properties: correlation with EGFR status.

  2005cited by this paper
• 2-(Quinazolin-4-ylamino)-[1,4]benzoquinones as covalent-binding, irreversible inhibitors of the kinase domain of vascular endothelial growth factor receptor-2.

  2005cited by this paper
• Anticancer therapeutics: "Addictive" targets, multi-targeted drugs, new drug combinations.

  2005cited by this paper
• Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl.

  2005cited by this paper
• Designed multiple ligands. An emerging drug discovery paradigm.

  2005cited by this paper
• Inhibition of homologous recombination by variants of the catalytic subunit of the DNA-dependent protein kinase (DNA-PKcs).

  2005cited by this paper
• Lysosomes as targets for cancer therapy.

  2005cited by this paper
• Role of the vascular endothelial growth factor pathway in tumor growth and angiogenesis.

  2005cited by this paper
• Mechanism of action of a novel "combi-triazene" engineered to possess a polar functional group on the alkylating moiety: evidence for enhancement of potency.

  2005cited by this paper
• Cytokinetics and mechanism of action of AKO4: a novel nitrogen mustard targeted to bcr-abl.

  2005cited by this paper
• Novel thiazonaphthalimides as efficient antitumor and DNA photocleaving agents: effects of intercalation, side chains, and substituent groups.

  2005cited by this paper
• Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib.

  2005cited by this paper
• Multiple mechanisms of action of ZR2002 in human breast cancer cells: A novel combi‐molecule designed to block signaling mediated by the ERB family of oncogenes and to damage genomic DNA

  2004cited by this paper
• Sequence‐specific potentiation of topoisomerase II inhibitors by the histone deacetylase inhibitor suberoylanilide hydroxamic acid

  2004cited by this paper
• The combi-targetinG concept: intracellular fragmentation of the binary epidermal growth factor (EGFR)/DNA targeting "combi-triazene" SMA41.

  2004cited by this paper
• Sustained antiproliferative mechanisms by RB24, a targeted precursor of multiple inhibitors of epidermal growth factor receptor and a DNA alkylating agent in the A431 epidermal carcinoma of the vulva cell line

  2004cited by this paper
• Antitumor Activity of ZD6474, a Vascular Endothelial Growth Factor Receptor Tyrosine Kinase Inhibitor, in Human Cancer Cells with Acquired Resistance to Antiepidermal Growth Factor Receptor Therapy

  2004cited by this paper
• Targeted cancer therapy

  2004cited by this paper
• The Combi-Targeting Concept: Dissection of the Binary Mechanism of Action of the Combi-Triazene SMA41 in Vitro and Antitumor Activity in Vivo

  2004cited by this paper
• From magic bullets to designed multiple ligands.

  2004cited by this paper
• The efficiency of multi-target drugs: the network approach might help drug design.

  2004cited by this paper
• Inhibition of cell signaling by the combi‐nitrosourea FD137 in the androgen independent DU145 prostate cancer cell line

  2004cited by this paper
• Synthesis of a prodrug designed to release multiple inhibitors of the epidermal growth factor receptor tyrosine kinase and an alkylating agent: a novel tumor targeting concept.

  2003cited by this paper
• The combi-targeting concept: chemical dissection of the dual targeting properties of a series of "combi-triazenes".

  2003cited by this paper
• Inhibition of histone deacetylase increases cytotoxicity to anticancer drugs targeting DNA.

  2003cited by this paper
• Histone deacetylase inhibitor LAQ824 both lowers expression and promotes proteasomal degradation of Bcr-Abl and induces apoptosis of imatinib mesylate-sensitive or -refractory chronic myelogenous leukemia-blast crisis cells.

  2003cited by this paper
• N-methylation of anthracyclines modulates their cytotoxicity and pharmacokinetic in wild type and multidrug resistant cells.

  2003cited by this paper
• Systematic discovery of multicomponent therapeutics

  2003cited by this paper
• The combi-targeting concept: a novel 3,3-disubstituted nitrosourea with EGFR tyrosine kinase inhibitory properties

  2002cited by this paper
• Inhibition of Epidermal Growth Factor Receptor-Mediated Signaling by “Combi-Triazene” BJ2000, a New Probe for Combi-Targeting Postulates

  2002cited by this paper
• DNA and its associated processes as targets for cancer therapy

  2002cited by this paper
• Differential responses of EGFR-/AGT-expressing cells to the "combi-triazene" SMA41

  2002cited by this paper
• Design of a chimeric 3-methyl-1,2,3-triazene with mixed receptor tyrosine kinase and DNA damaging properties: a novel tumor targeting strategy.

  2001cited by this paper
• Intercalators as anticancer drugs.

  2001cited by this paper

• A glycosylated naphthalimide conjugate preferentially accumulates in metastatic hepatocellular carcinoma as ROS-mediated mitochondrial-targeted antimetastatic agent

  2025cites this paper
• Fluorescent Peptide-Containing Naphthalimide-Conjugated Boronic Acid-Based Nanoassembly for Rapid Mitochondrial Targeting and Antibacterial Activity.

  2025cites this paper
• LAMP2-Mediated Autophagy Plasticity Deters Lysosomal Uptake of Platinum Ions to Reverse Cisplatin-Induced Glioma Progression in a Macrophage Dependent Manner.

  2025cites this paper
• Synthesis, biological and pharmacokinetic characterization of a novel leucine ureido derivative as a multi-target anticancer agent

  2025cites this paper
• Discovery of Diaryl Piperidone-Sulfonamide as a Novel Dual-Target Inhibitor of STAT3/CAIX Inducing Ferroptosis in Triple-Negative Breast Cancer Cells.

  2025cites this paper
• Investigating the Antibacterial Efficiency and Mechanism of Indole- and Naphthalimide-Mediated Benzimidazoles: Membrane Damage, Metabolic Inactivation, and Oxidative Stress against Bacillus subtilis.

  2025cites this paper
• Privileged Scaffold Hybridization in the Design of Carbonic Anhydrase Inhibitors

  2024cites this paper
• A Review on the Anticancer Activity of Carbazole-based Tricyclic Compounds.

  2023cites this paper
• Synthesis of 4,5-Dihydro-1H-[1,2]dithiolo[3,4-c]quinoline-1-thione Derivatives and Their Application as Protein Kinase Inhibitors

  2022cites this paper
• Recent developments on 1,8-Naphthalimide moiety as potential target for anticancer agents.

  2022cites this paper
• An unanticipated discovery of novel naphthalimidopropanediols as potential broad-spectrum antibacterial members.

  2022cites this paper
• New Series of Pyrazoles and Imidazo-Pyrazoles Targeting Different Cancer and Inflammation Pathways

  2021cites this paper
• Development of the phenylpyrazolo[3,4-d]pyrimidine-based, insulin-like growth factor receptor/Src/AXL-targeting small molecule kinase inhibitor

  2021cites this paper
• A naphthalimide-polyamine conjugate preferentially accumulates in hepatic carcinoma metastases as a lysosome-targeted antimetastatic agent.

  2021cites this paper
• An unanticipated discovery towards novel naphthalimide corbelled aminothiazoximes as potential anti-MRSA agents and allosteric modulators for PBP2a.

  2021cites this paper
• Hybrid Anticancer Peptides DN1 and DN4 Exert Selective Cytotoxicity Against Hepatocellular Carcinoma Cells by Inducing Both Intrinsic and Extrinsic Apoptotic Pathways

  2021cites this paper
• Transferrin receptors targeting peptide (T7 peptide) surface-modified sorafenib nanoliposomes enhance the anti-tumor effect in colorectal cancer

  2020cites this paper
• Molecular modeling and LC–MS-based metabolomics of a glutamine-valproic acid (Gln-VPA) derivative on HeLa cells

  2020cites this paper
• A Polyamine-Based Dinitro-Naphthalimide Conjugate as Substrates for Polyamine Transporters Preferentially Accumulates in Cancer Cells and Minimizes Side Effects in vitro and in vivo

  2020cites this paper
• Chemogenomics and bioinformatics approaches for prioritizing kinases as drug targets for neglected tropical diseases.

  2020cites this paper
• Perspectives on Drug Repurposing.

  2020cites this paper
• A Pt(IV)-based mononitro-naphthalimide conjugate with minimized side-effects targeting DNA damage response via a dual-DNA-damage approach to overcome cisplatin resistance.

  2020cites this paper
• Breast Cancer Chemotherapeutic Options: A General Overview on the Preclinical Validation of a Multi-Target Ruthenium(III) Complex Lodged in Nucleolipid Nanosystems

  2020cites this paper
• Transferrin Modified Nano-liposome Co-delivery Strategies for Enhancing the Cancer Therapy.

  2019cites this paper
• Design, synthesis and cytotoxicity of chimeric erlotinib-alkylphospholipid hybrids.

  2019cites this paper
• Memantine prodrug as a new agent for Alzheimer’s Disease

  2019cites this paper
• Dual-targeted hit identification using pharmacophore screening

  2019cites this paper
• Drug Repurposing for Cancer Therapy, Easier Said Than Done.

  2019cites this paper
• Exploiting polypharmacology for improving therapeutic outcome of kinase inhibitors (KIs): An update of recent medicinal chemistry efforts.

  2018cites this paper
• New Multitarget Approaches in the War Against Glioblastoma: A Mini-Perspective

  2018cites this paper
• Novel naphthalimide nitroimidazoles as multitargeting antibacterial agents against resistant Acinetobacter baumannii.

  2018cites this paper
• Synthesis and biological evaluation of naphthalimide-polyamine conjugates modified by alkylation as anticancer agents through p53 pathway.

  2018cites this paper
• Novel potentially antibacterial naphthalimide-derived metronidazoles: Design, synthesis, biological evaluation and supramolecular interactions with DNA, human serum albumin and topoisomerase II

  2017cites this paper
• Computational Methods in Multitarget Drug Discovery

  2017cites this paper
• Dianhydrogalactitol, a potential multitarget agent, inhibits glioblastoma migration, invasion, and angiogenesis.

  2017cites this paper
• Design, Synthesis, and Biological Evaluation of Mitochondria-Targeted Flavone-Naphthalimide-Polyamine Conjugates with Antimetastatic Activity.

  2017cites this paper
• Recent progress on curcumin-based therapeutics: a patent review (2012-2016). Part I: Curcumin

  2017cites this paper
• Discovery of Multi-target Anticancer Agents Based on HDAC Inhibitor MS-275 and 5-FU.

  2016cites this paper
• Synthesis and biological evaluation of Schiff base-linked imidazolyl naphthalimides as novel potential anti-MRSA agents

  2016cites this paper
• Heterocyclic Naphthalimides as New Skeleton Structure of Compounds with Increasingly Expanding Relational Medicinal Applications.

  2016cites this paper
• Development and Application of a Virtual Screening Protocol for the Identification of Multitarget Fragments

  2016cites this paper
• Multi-kinase inhibitors.

  2015cites this paper
• Novel benzimidazole derived naphthalimide triazoles: synthesis, antimicrobial activity and interactions with calf thymus DNA

  2015cites this paper
• pH-Sensitive carboxymethyl chitosan-modified cationic liposomes for sorafenib and siRNA co-delivery

  2015cites this paper
• Multifunctional compounds: smart molecules for multifactorial diseases.

  2014cites this paper
• The Acetylenic Tricyclic Bis(cyano enone), TBE-31 Inhibits Non–Small Cell Lung Cancer Cell Migration through Direct Binding with Actin

  2014cites this paper
• Caffeic acid derivatives, analogs and applications: a patent review (2009 – 2013)

  2014cites this paper
• Molecular aspects of resistance to biological and non-biological drugs and strategies to overcome resistance in colorectal cancer.

  2014cites this paper
• Complexity against complexity: multitarget drugs.

  2013cites this paper
• Human disease and drug pharmacology, complex as real life.

  2013cites this paper