Steric Blockade of Oxy-Myoglobin Oxidation by Thiosemicarbazones: Structure–Activity Relationships of the Novel PPP4pT Series

Designing Tailored Thiosemicarbazones with Bespoke Properties: The Styrene Moiety Imparts Potent Activity, Inhibits Heme Center Oxidation, and Results in a Novel “Stealth Zinc(II) Complex”

(2023) Mahendiran Dharmasivam et al.   Journal of Medicinal Chemistry

Dual Role of Glutathione as a Reducing Agent and Cu-Ligand Governs the ROS Production by Anticancer Cu-Thiosemicarbazone Complexes

(2023) Alessandra G. Ritacca et al.   Inorganic Chemistry

“Magic Chloro”: Profound Effects of the Chlorine Atom in Drug Discovery

(2023) Debora Chiodi et al.   Journal of Medicinal Chemistry

Developing a Multitargeted Anticancer Palladium(II) Agent Based on the His-242 Residue in the IIA Subdomain of Human Serum Albumin

(2023) Wenjuan Li et al.   Journal of Medicinal Chemistry

Developing a Gadolinium(III) Compound Based on Apoferritin for Targeted Magnetic Resonance Imaging and Dual-Modal Therapy of Cancer

(2023) Xueyu Man et al.   Journal of Medicinal Chemistry

The Myc Family and the Metastasis Suppressor NDRG1: Targeting Key Molecular Interactions with Innovative Therapeutics

(2023) Zhao Deng et al.   PHARMACOLOGICAL REVIEWS

Innovative thiosemicarbazones that induce multi-modal mechanisms to down-regulate estrogen-, progesterone-, androgen- and prolactin-receptors in breast cancer

(2023) Faten Shehadeh-Tout et al.   PHARMACOLOGICAL RESEARCH

Aqueous Iron(IV)–Oxo Complex: An Emerging Powerful Reactive Oxidant Formed by Iron(II)-Based Advanced Oxidation Processes for Oxidative Water Treatment

(2022) Zhen Wang et al.   ENVIRONMENTAL SCIENCE & TECHNOLOGY

Discovery of new PKN2 inhibitory chemotypes via QSAR-guided selection of docking-based pharmacophores

(2022) Mahmoud A. Al-Sha’er et al.   MOLECULAR DIVERSITY

The thiosemicarbazone, DpC, broadly synergizes with multiple anti-cancer therapeutics and demonstrates temperature- and energy-dependent uptake by tumor cells

(2022) Mahendiran Dharmasivam et al.   BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS

Copper-Catalyzed Glutathione Oxidation is Accelerated by the Anticancer Thiosemicarbazone Dp44mT and Further Boosted at Lower pH

(2022) Enrico Falcone et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

An efficient ultrasound-assisted CH3COONa catalyzed synthesis of thiazolidinone molecule: Theoretical and nonlinear optical evaluations of thiazolidinone-Schiff base derivative

(2022) Jinan Khudhair Salim et al.   OPTICAL MATERIALS

Targeting Mutant p53 for Cancer Treatment: Moving Closer to Clinical Use?

(2022) Michael J. Duffy et al.   Cancers

Thiosemicarbazone Derivatives Developed to Overcome COTI-2 Resistance

(2022) Vivien Pósa et al.   Cancers

Breaking the cycle: Targeting of NDRG1 to inhibit bi‐directional oncogenic cross‐talk between pancreatic cancer and stroma

(2021) Bekesho Geleta et al.   FASEB JOURNAL

Benzothiazolyl and Benzoxazolyl Hydrazones Function as Zinc Metallochaperones to Reactivate Mutant p53

(2021) John A. Gilleran et al.   JOURNAL OF MEDICINAL CHEMISTRY

Innovative Therapies for Neuroblastoma: The Surprisingly Potent Role of Iron Chelation in Up-Regulating Metastasis and Tumor Suppressors and Down-Regulating the Key Oncogene, N-myc

(2021) Tharushi P. Wijesinghe et al.   PHARMACOLOGICAL RESEARCH

The Oncogenic Signaling Disruptor, NDRG1: Molecular and Cellular Mechanisms of Activity

(2021) Jason Chekmarev et al.   Cells

Design, Synthesis, Biological Evaluation, and Computational Studies of Novel Fluorinated Candidates as PI3K Inhibitors: Targeting Fluorophilic Binding Sites

(2021) Ahmed H. Tantawy et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, In Silico Study, and Anti-Cancer Activity of Thiosemicarbazone Derivatives

(2021) Belay Zeleke Sibuh et al.   Biomedicines

Unique targeting of androgen‐dependent and ‐independent AR signaling in prostate cancer to overcome androgen resistance

(2020) Syer C. Lim et al.   FASEB JOURNAL

Cancer Cell Resistance Against the Clinically Investigated Thiosemicarbazone COTI-2 Is Based on Formation of Intracellular Copper Complex Glutathione Adducts and ABCC1-Mediated Efflux

(2020) Julia H. Bormio Nunes et al.   JOURNAL OF MEDICINAL CHEMISTRY

COTI-2, a novel thiosemicarbazone derivative, exhibits antitumor activity in HNSCC through p53-dependent and -independent mechanisms

(2019) Antje Lindemann et al.   CLINICAL CANCER RESEARCH

Synthetic approaches and pharmaceutical applications of chloro-containing molecules for drug discovery: A critical review

(2019) Wan-Yin Fang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

PEG-conjugated triacontanol micelles as docetaxel delivery systems for enhanced anti-cancer efficacy

(2019) Xiaoyu Lu et al.   Drug Delivery and Translational Research

Randomized Phase II Trial of Triapine-Cisplatin-Radiotherapy for Locally Advanced Stage Uterine Cervix or Vaginal Cancers

(2019) Charles A. Kunos et al.   Frontiers in Oncology

Autodock Vina Adopts More Accurate Binding Poses but Autodock4 Forms Better Binding Affinity

(2019) Nguyen Thanh Nguyen et al.   Journal of Chemical Information and Modeling

Anticancer Thiosemicarbazones: Chemical Properties, Interaction with Iron Metabolism, and Resistance Development

(2018) Petra Heffeter et al.   ANTIOXIDANTS & REDOX SIGNALING

Investigation of the Redox and Acid-Base properties of TCNQF and TCNQF2 : Electrochemistry, Vibrational Spectroscopy, and Substituent Effects

(2018) Nguyen Vo et al.   ChemElectroChem

Abstract CT033: Safety and early efficacy signals for COTI-2, an orally available small molecule targeting p53, in a phase I trial of recurrent gynecologic cancer

(2018) Shannon N. Westin et al.   CANCER RESEARCH

Effect of Inflammatory Mediators Lipopolysaccharide and Lipoteichoic Acid on Iron Metabolism of Differentiated SH-SY5Y Cells Alters in the Presence of BV-2 Microglia

(2018) Edina Pandur et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Using droplet digital PCR to analyze MYCN and ALK copy number in plasma from patients with neuroblastoma

(2017) Marco Lodrini et al.   Oncotarget

Phase I trial of daily triapine in combination with cisplatin chemotherapy for advanced-stage malignancies

(2016) Charles A. Kunos et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

COTI-2, a new anticancer drug currently under clinical investigation, targets mutant p53 and negatively modulates the PI3K/AKT/mTOR pathway

(2016) K.Y. Salim et al.   EUROPEAN JOURNAL OF CANCER

The novel thiosemicarbazone, di-2-pyridylketone 4-cyclohexyl-4-methyl-3-thiosemicarbazone (DpC), inhibits neuroblastoma growth in vitro and in vivo via multiple mechanisms

(2016) Zhu-Ling Guo et al.   Journal of Hematology & Oncology

Kinetico-mechanistic studies on methemoglobin generation by biologically active thiosemicarbazone iron(III) complexes

(2016) Maram T. Basha et al.   JOURNAL OF INORGANIC BIOCHEMISTRY

Zinc(II)–Thiosemicarbazone Complexes Are Localized to the Lysosomal Compartment Where They Transmetallate with Copper Ions to Induce Cytotoxicity

(2016) Alexandra E. Stacy et al.   JOURNAL OF MEDICINAL CHEMISTRY

A mechanism for overcoming P-glycoprotein-mediated drug resistance: novel combination therapy that releases stored doxorubicin from lysosomes via lysosomal permeabilization using Dp44mT or DpC

(2016) Nicole A Seebacher et al.   Cell Death & Disease

COTI-2, a novel small molecule that is active against multiple human cancer cell lines in vitro and in vivo

(2016) Kowthar Y. Salim et al.   Oncotarget

Nano-curcumin prepared via supercritical: Improved anti-bacterial, anti-oxidant and anti-cancer efficacy

(2015) Maobin Xie et al.   INTERNATIONAL JOURNAL OF PHARMACEUTICS

Di-2-pyridylketone 4,4-Dimethyl-3-thiosemicarbazone (Dp44mT) Overcomes Multidrug Resistance by a Novel Mechanism Involving the Hijacking of Lysosomal P-Glycoprotein (Pgp)

(2015) Patric J. Jansson et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Glucose Modulation Induces Lysosome Formation and Increases Lysosomotropic Drug Sequestration via the P-Glycoprotein Drug Transporter

(2015) Nicole A. Seebacher et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Novel Mechanism of Cytotoxicity for the Selective Selenosemicarbazone, 2-Acetylpyridine 4,4-Dimethyl-3-selenosemicarbazone (Ap44mSe): Lysosomal Membrane Permeabilization

(2015) Zaynab Al-Eisawi et al.   JOURNAL OF MEDICINAL CHEMISTRY

The renaissance of polypharmacology in the development of anti-cancer therapeutics: Inhibition of the “Triad of Death” in cancer by Di-2-pyridylketone thiosemicarbazones

(2015) Patric J. Jansson et al.   PHARMACOLOGICAL RESEARCH

Novel and potent anti-tumor and anti-metastatic di-2-pyridylketone thiosemicarbazones demonstrate marked differences in pharmacology between the first and second generation lead agents

(2015) Vit Sestak et al.   Oncotarget

Thiosemicarbazide, a fragment with promising indolamine-2,3-dioxygenase (IDO) inhibition properties

(2014) Silvia Serra et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

The metastasis suppressor NDRG1 modulates the phosphorylation and nuclear translocation of  -catenin through mechanisms involving FRAT1 and PAK4

(2014) R. Jin et al.   JOURNAL OF CELL SCIENCE

Kinetic studies on the oxidation of oxyhemoglobin by biologically active iron thiosemicarbazone complexes: relevance to iron-chelator-induced methemoglobinemia

(2013) Maram T. Basha et al.   JOURNAL OF BIOLOGICAL INORGANIC CHEMISTRY

Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings

(2012) Christopher A. Lipinski et al.   ADVANCED DRUG DELIVERY REVIEWS

Novel Chelators for Cancer Treatment: Where Are We Now?

(2012) Angelica M. Merlot et al.   ANTIOXIDANTS & REDOX SIGNALING

Design of iron chelators with therapeutic application

(2012) Tao Zhou et al.   DALTON TRANSACTIONS

N-myc downstream regulated gene 1 modulates Wnt-β-catenin signalling and pleiotropically suppresses metastasis

(2012) Wen Liu et al.   EMBO Molecular Medicine

The Iron Chelators Dp44mT and DFO Inhibit TGF-β-induced Epithelial-Mesenchymal Transition via Up-Regulation of N-Myc Downstream-regulated Gene 1 (NDRG1)

(2012) Zhiqiang Chen et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Novel Second-Generation Di-2-Pyridylketone Thiosemicarbazones Show Synergism with Standard Chemotherapeutics and Demonstrate Potent Activity against Lung Cancer Xenografts after Oral and Intravenous Administration in Vivo

(2012) David B. Lovejoy et al.   JOURNAL OF MEDICINAL CHEMISTRY

Simple pyrazoline and pyrazole “turn on” fluorescent sensors selective for Cd2+ and Zn2+ in MeCN

(2012) Alexander Ciupa et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Evidence of asymmetric cell division and centrosome inheritance in human neuroblastoma cells

(2012) H. Izumi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Bp44mT: an orally active iron chelator of the thiosemicarbazone class with potent anti-tumour efficacy

(2011) Y Yu et al.   BRITISH JOURNAL OF PHARMACOLOGY

Antitumor Activity of Metal-Chelating Compound Dp44mT Is Mediated by Formation of a Redox-Active Copper Complex That Accumulates in Lysosomes

(2011) D. B. Lovejoy et al.   CANCER RESEARCH

What has polar surface area ever done for drug discovery?

(2011) David E Clark   Future Medicinal Chemistry

Novel Thiosemicarbazone Iron Chelators Induce Up-Regulation and Phosphorylation of the Metastasis Suppressor N-myc Down-Stream Regulated Gene 1: A New Strategy for the Treatment of Pancreatic Cancer

(2011) Z. Kovacevic et al.   MOLECULAR PHARMACOLOGY

Novel Thiosemicarbazones of the ApT and DpT Series and Their Copper Complexes: Identification of Pronounced Redox Activity and Characterization of Their Antitumor Activity

(2010) Patric J. Jansson et al.   JOURNAL OF MEDICINAL CHEMISTRY

A phase II trial of Triapine® (NSC# 663249) and gemcitabine as second line treatment of advanced non-small cell lung cancer: Eastern Cooperative Oncology Group Study 1503

(2009) Anne M. Traynor et al.   INVESTIGATIONAL NEW DRUGS

AutoDock4 and AutoDockTools4: Automated docking with selective receptor flexibility

(2009) Garrett M. Morris et al.   JOURNAL OF COMPUTATIONAL CHEMISTRY

2-Acetylpyridine Thiosemicarbazones are Potent Iron Chelators and Antiproliferative Agents: Redox Activity, Iron Complexation and Characterization of their Antitumor Activity

(2009) Des R. Richardson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Antitumor activity and mechanism of action of the iron chelator, Dp44mT, against leukemic cells

(2008) Egarit Noulsri et al.   AMERICAN JOURNAL OF HEMATOLOGY

Cancer cell iron metabolism and the development of potent iron chelators as anti-tumour agents

(2008) D.R. Richardson et al.   BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS

Iron Chelators of the Dipyridylketone Thiosemicarbazone Class: Precomplexation and Transmetalation Effects on Anticancer Activity

(2008) Paul V. Bernhardt et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Cytosolic Iron Chaperone That Delivers Iron to Ferritin

(2008) H. Shi et al.   SCIENCE