Acridine and its derivatives: a patent review (2009 – 2013)

Use of Yeast Chemigenomics and COXEN Informatics in Preclinical Evaluation of Anticancer Agents

(2015) Steven C. Smith et al.   NEOPLASIA

Natural and synthetic acridines/acridones as antitumor agents: their biological activities and methods of synthesis

(2014) Grzegorz Cholewiński et al.   Pharmacological Reports

Small Targeted Cytotoxics: Current State and Promises from DNA-Encoded Chemical Libraries

(2013) Nikolaus Krall et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Combination of fludarabine, amsacrine, and cytarabine followed by reduced-intensity conditioning and allogeneic hematopoietic stem cell transplantation in patients with high-risk acute myeloid leukemia

(2013) Marta Krejci et al.   ANNALS OF HEMATOLOGY

Protein recognition of the S23906-1–DNA adduct by nuclear proteins: direct involvement of glyceraldehyde-3-phosphate dehydrogenase (GAPDH)

(2013) Gaëlle Lenglet et al.   BIOCHEMICAL JOURNAL

Pregnane X receptor dependent up-regulation of CYP2C9 and CYP3A4 in tumor cells by antitumor acridine agents, C-1748 and C-1305, selectively diminished under hypoxia

(2013) Magdalena Niemira et al.   BIOCHEMICAL PHARMACOLOGY

Novel synthetic acridine derivatives as potent DNA-binding and apoptosis-inducing antitumor agents

(2013) Xuliang Lang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

PT-ACRAMTU, A Platinum–Acridine Anticancer Agent, Lengthens and Aggregates, but does not Stiffen or Soften DNA

(2013) Samrat Dutta et al.   CELL BIOCHEMISTRY AND BIOPHYSICS

Design of a platinum–acridine–endoxifen conjugate targeted at hormone-dependent breast cancer

(2013) Song Ding et al.   CHEMICAL COMMUNICATIONS

Sequestration of AS-DACA into Acidic Compartments of the Membrane Trafficking System as a Mechanism of Drug Resistance in Rhabdomyosarcoma

(2013) Marissa Williams et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

High-Dose Cytarabine Consolidation With or Without Additional Amsacrine and Mitoxantrone in Acute Myeloid Leukemia: Results of the Prospective Randomized AML2003 Trial

(2013) Markus Schaich et al.   JOURNAL OF CLINICAL ONCOLOGY

Niche for Acridine Derivatives in Anticancer Therapy

(2013) Galdino-Pitta R. et al.   MINI-REVIEWS IN MEDICINAL CHEMISTRY

Synthesis, kinetic studies and molecular modeling of novel tacrine dimers as cholinesterase inhibitors

(2013) Roney Anderson Nascimento de Aquino et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Inhibition of DNA topoisomerase I activity and induction of apoptosis by thiazacridine derivatives

(2013) Francisco W.A. Barros et al.   TOXICOLOGY AND APPLIED PHARMACOLOGY

Enhanced Antiproliferative Activity of the New Anticancer Candidate LPSF/AC04 in Cyclodextrin Inclusion Complexes Encapsulated into Liposomes

(2012) Elisângela A. M. Mendonça et al.   AAPS PHARMSCITECH

Comparative Chemogenomics To Examine the Mechanism of Action of DNA-Targeted Platinum-Acridine Anticancer Agents

(2012) Kahlin Cheung-Ong et al.   ACS Chemical Biology

CYP3A4 overexpression enhances the cytotoxicity of the antitumor triazoloacridinone derivative C-1305 in CHO cells

(2012) Ewa Augustin et al.   ACTA PHARMACOLOGICA SINICA

PARP inhibition potentiates the cytotoxic activity of C-1305, a selective inhibitor of topoisomerase II, in human BRCA1-positive breast cancer cells

(2012) Józefa Węsierska-Gądek et al.   BIOCHEMICAL PHARMACOLOGY

Amsacrine as a Topoisomerase II Poison: Importance of Drug–DNA Interactions

(2012) Adam C. Ketron et al.   BIOCHEMISTRY

Synthesis and cytotoxic activity of new acridine-thiazolidine derivatives

(2012) Francisco W.A. Barros et al.   BIOORGANIC & MEDICINAL CHEMISTRY

DNA Metalating-Intercalating Hybrid Agents for the Treatment of Chemoresistant Cancers

(2012) Jimmy Suryadi et al.   CHEMISTRY-A EUROPEAN JOURNAL

Synthesis, Aqueous Reactivity, and Biological Evaluation of Carboxylic Acid Ester-Functionalized Platinum–Acridine Hybrid Anticancer Agents

(2012) Leigh A. Graham et al.   JOURNAL OF MEDICINAL CHEMISTRY

Using a Build-and-Click Approach for Producing Structural and Functional Diversity in DNA-Targeted Hybrid Anticancer Agents

(2012) Song Ding et al.   JOURNAL OF MEDICINAL CHEMISTRY

Tacrine–Ferulic Acid–Nitric Oxide (NO) Donor Trihybrids as Potent, Multifunctional Acetyl- and Butyrylcholinesterase Inhibitors

(2012) Yao Chen et al.   JOURNAL OF MEDICINAL CHEMISTRY

New Tacrine–4-Oxo-4H-chromene Hybrids as Multifunctional Agents for the Treatment of Alzheimer’s Disease, with Cholinergic, Antioxidant, and β-Amyloid-Reducing Properties

(2012) María Isabel Fernández-Bachiller et al.   JOURNAL OF MEDICINAL CHEMISTRY

Assessment of amsacrine binding with DNA using UV–visible, circular dichroism and Raman spectroscopic techniques

(2012) Deepak Kumar Jangir et al.   JOURNAL OF PHOTOCHEMISTRY AND PHOTOBIOLOGY B-BIOLOGY

Synthesis and in vitro anticancer activity of novel thiazacridine derivatives

(2012) Marina Galdino da Rocha Pitta et al.   MEDICINAL CHEMISTRY RESEARCH

Analysis of the DNA damage produced by a platinum–acridine antitumor agent and its effects in NCI-H460 lung cancer cells

(2012) Xin Qiao et al.   Metallomics

Effects of a tacrine-8-hydroxyquinoline hybrid (IQM-622) on Aβ accumulation and cell death: Involvement in hippocampal neuronal loss in Alzheimer's disease

(2012) Desiree Antequera et al.   NEUROBIOLOGY OF DISEASE

Tacrine-6-Ferulic Acid, a Novel Multifunctional Dimer, Inhibits Amyloid-β-Mediated Alzheimer's Disease-Associated Pathogenesis In Vitro and In Vivo

(2012) Rongbiao Pi et al.   PLoS One

Synthesis and evaluation of 10-(3,5-dimethoxy)benzyl-9(10H)-acridone derivatives as selective telomeric G-quadruplex DNA ligands

(2012) Chunmei Gao et al.   TETRAHEDRON

Solvent- and chromatography-free amination of π-deficient nitrogen heterocycles under microwave irradiation. A fast, efficient and green route to 9-aminoacridines, 4-aminoquinolines and 4-aminoquinazolines and its application to the synthesis of the drugs amsacrine and bistacrine

(2012) Matteo Staderini et al.   TETRAHEDRON

Pre-clinical pharmacokinetics of the acridine antitumour candidate AC04 and its 1-oxo-metabolite plasma profile

(2012) Maiara Cássia Pigatto et al.   XENOBIOTICA

Two-in-one: a pH-sensitive, acridine-based, fluorescent probe binds G-quadruplexes in oncogene promoters

(2012) Claudia Percivalle et al.   MedChemComm

Exploration of acridine scaffold as a potentially interesting scaffold for discovering novel multi-target VEGFR-2 and Src kinase inhibitors

(2011) Xudong Luan et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Intracellular trafficking as a determinant of AS-DACA cytotoxicity in rhabdomyosarcoma cells

(2011) Steven J Wolf et al.   BMC CELL BIOLOGY

Novel activity of acriflavine against colorectal cancer tumor cells

(2011) Saadia Hassan et al.   CANCER SCIENCE

Novel Synthetic Azaacridine Analogues as Topoisomerase 1 Inhibitors

(2011) Xudong Luan et al.   CHEMISTRY LETTERS

The Imidazoacridinone Antitumor Drug, C-1311, Is Metabolized by Flavin Monooxygenases but Not by Cytochrome P450s

(2011) A. Potega et al.   DRUG METABOLISM AND DISPOSITION

Synthesis and cytotoxic activity of benzo[a]acronycine and benzo[b]acronycine substituted on the A ring

(2011) Thomas Gaslonde et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Antineoplastic activity of the thiazolo[5,4-b]quinoline derivative D3CLP in K-562 cells is mediated through effector caspases activation

(2011) Ignacio González-Sánchez et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Metabolism evaluation of the anticancer candidate AC04 by biomimetic oxidative model and rat liver microsomes

(2011) Maiara Cássia Pigatto et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

DEVELOPMENT AND VALIDATION OF AN LC-MS/MS METHOD FOR THE PRE-CLINICAL PHARMACOKINETIC INVESTIGATION OF THE ANTICANCER CANDIDATE AC04 IN RODENTS

(2011) Flávia De Toni Uchôa et al.   JOURNAL OF LIQUID CHROMATOGRAPHY & RELATED TECHNOLOGIES

Huprine–Tacrine Heterodimers as Anti-Amyloidogenic Compounds of Potential Interest against Alzheimer’s and Prion Diseases

(2011) Carles Galdeano et al.   JOURNAL OF MEDICINAL CHEMISTRY

Tröger’s bases in the acronycine, benzo[a]acronycine, and benzo[b]acronycine series

(2011) Thomas Gaslonde et al.   TETRAHEDRON LETTERS

Synthesis and in vivo evaluation of 18F-fluoroethyl GF120918 and XR9576 as positron emission tomography probes for assessing the function of drug efflux transporters

(2010) Kazunori Kawamura et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design, synthesis and evaluation of novel tacrine-multialkoxybenzene hybrids as dual inhibitors for cholinesterases and amyloid beta aggregation

(2010) Wen Luo et al.   BIOORGANIC & MEDICINAL CHEMISTRY

New Synthetic Routes to Acronycine, Noracronycine, and Their Analogues

(2010) Galla Sri Hari et al.   BULLETIN OF THE KOREAN CHEMICAL SOCIETY

Probing Platinum−Adenine-N3 Adduct Formation with DNA Minor-Groove Binding Agents

(2010) Lu Rao et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Physicochemical interaction of antitumor acridinone derivatives with DNA in view of QSAR studies

(2010) Marcin Koba et al.   MEDICINAL CHEMISTRY RESEARCH

Evaluation of Limiting Brain Penetration Related to P-glycoprotein and Breast Cancer Resistance Protein Using [11C]GF120918 by PET in Mice

(2010) Kazunori Kawamura et al.   MOLECULAR IMAGING AND BIOLOGY

The P-glycoprotein Inhibitor GF120918 Modulates Ca2+-Dependent Processes and Lipid Metabolism in Toxoplasma Gondii

(2010) Iveta Bottova et al.   PLoS One

G-quadruplex compounds and cis-platin act synergistically to inhibit cancer cell growth in vitro and in vivo

(2009) Mekala Gunaratnam et al.   BIOCHEMICAL PHARMACOLOGY

Synthesis, cytotoxic activity, and DNA binding properties of antitumor cis-1,2-dihydroxy-1,2-dihydrobenzo[b]acronycine cinnamoyl esters

(2009) Quyên Do et al.   BIOORGANIC & MEDICINAL CHEMISTRY

In vitro assessment of novel transcription inhibitors and topoisomerase poisons in rhabdomyosarcoma cell lines

(2009) Steven J. Wolf et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Synthesis and cytotoxic activity of psorospermin and acronycine analogues in the 3-propyloxy-acridin-9(10 H )-one and -benzo[ b ]acridin-12(5 H )-one series

(2009) Sabrina Boutefnouchet et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Human telomeric G-quadruplex: The current status of telomeric G-quadruplexes as therapeutic targets in human cancer

(2009) Stephen Neidle   FEBS Journal

Phase II trial of pyrazoloacridine (NSC#366140) in patients with metastatic breast cancer

(2009) Bhuvaneswari Ramaswamy et al.   INVESTIGATIONAL NEW DRUGS

Involvement of ATM-mediated Chk1/2 and JNK kinase signaling activation in HKH40A-induced cell growth inhibition

(2009) Ziqiu Wang et al.   JOURNAL OF CELLULAR PHYSIOLOGY

Structural Investigations of Acridine Derivatives by CoMFA and CoMSIA Reveal Novel Insight into Their Structures toward DNA G-Quadruplex Mediated Telomerase Inhibition and Offer a Highly Predictive 3D-Model for Substituted Acridines

(2009) Vishal P. Zambre et al.   Journal of Chemical Information and Modeling

Influence of the Stereoisomeric Position of the Reactive Acetate Groups of the Benzo[b]Acronycine derivative S23906-1 on Its DNA Alkylation, Helix-Opening, Cytotoxic, and Antitumor Activities

(2009) S. Depauw et al.   MOLECULAR PHARMACOLOGY

Synthesis and antitumor activity of novel amsacrine analogs: The critical role of the acridine moiety in determining their biological activity

(2008) Adriana Chilin et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Growth inhibition of hepatocellular carcinoma cells in vitro and in vivo by the 8-methoxy analog of WMC79

(2008) Teresa Kosakowska-Cholody et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Acridine/acridone: a simple scaffold with a wide range of application in oncology

(2008) Philippe Belmont et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Formulation and pharmacokinetic evaluation of an asulacrine nanocrystalline suspension for intravenous delivery

(2008) Srinivas Ganta et al.   INTERNATIONAL JOURNAL OF PHARMACEUTICS

Structural Basis of DNA Quadruplex Recognition by an Acridine Drug

(2008) Nancy H. Campbell et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY