Advances in thiosemicarbazone metal complexes as anti-lung cancer agents

XG Bai, Y Zheng, J Qi - Frontiers in Pharmacology, 2022 - frontiersin.org
The great success of cisplatin as a chemotherapeutic agent considerably increased
research efforts in inorganic biochemistry to identify more metallic drugs having the potential …

The myc family and the metastasis suppressor NDRG1: targeting key molecular interactions with innovative therapeutics

Z Deng, DR Richardson, P Insel - Pharmacological Reviews, 2023 - Elsevier
Cancer is a leading cause of death worldwide, resulting in∼ 10 million deaths in 2020.
Major oncogenic effectors are the Myc proto-oncogene family, which consists of three …

Isosteric Replacement of Sulfur to Selenium in a Thiosemicarbazone: Promotion of Zn (II) Complex Dissociation and Transmetalation to Augment Anticancer Efficacy

B Kaya, M Gholam Azad, M Suleymanoglu… - Journal of Medicinal …, 2024 - ACS Publications
We implemented isosteric replacement of sulfur to selenium in a novel thiosemicarbazone
(PPTP4c4mT) to create a selenosemicarbazone (PPTP4c4mSe) that demonstrates …

Targeting lysosomes by design: novel N-acridine thiosemicarbazones that enable direct detection of intracellular drug localization and overcome P-glycoprotein (Pgp) …

B Kaya, H Smith, Y Chen, MG Azad, TM Russell… - Chemical …, 2024 - pubs.rsc.org
Innovative N-acridine thiosemicarbazones (NATs) were designed along with their iron (III),
copper (II), and zinc (II) complexes. Lysosomal targeting was promoted by specifically …

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

TP Wijesinghe, B Kaya, MA Gonzálvez… - Journal of Medicinal …, 2023 - ACS Publications
The di-2-pyridylketone thiosemicarbazones demonstrated marked anticancer efficacy,
prompting progression of DpC to clinical trials. However, DpC induced deleterious oxy …

Differential transmetallation of complexes of the anti-cancer thiosemicarbazone, Dp4e4mT: effects on anti-proliferative efficacy, redox activity, oxy-myoglobin and oxy …

M Dharmasivam, B Kaya, TP Wijesinghe… - Chemical …, 2024 - pubs.rsc.org
The di-2-pyridylthiosemicarbazone (DpT) analogs demonstrate potent and selective anti-
proliferative activity against human tumors. The current investigation reports the synthesis …

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

F Shehadeh-Tout, HH Milioli, S Roslan… - Pharmacological …, 2023 - Elsevier
The estrogen receptor-α (ER-α) is a key driver of breast cancer (BC) and the ER-antagonist,
tamoxifen, is a central pillar of BC treatment. However, cross-talk between ER-α, other …

Targeting iron to contrast cancer progression

E Tomat - Current opinion in chemical biology, 2023 - Elsevier
An altered metabolism of iron fuels cancer growth, invasion, metastasis, and recurrence.
Ongoing research in cancer biology is delineating a complex iron-trafficking program …

Thiosemicarbazone-benzenesulfonamide Derivatives as Human Carbonic Anhydrases Inhibitors: Synthesis, Characterization, and In silico Studies

M Trawally, K Demir-Yazıcı, A Angeli… - Anti-Cancer Agents …, 2024 - benthamdirect.com
Introduction: Carbonic anhydrases (CAs) are widespread metalloenzymes with the core
function of catalyzing the interconversion of CO2 and HCO3-. Targeting these enzymes …

Innovative N-Acridine Thiosemicarbazones and Their Zn(II) Complexes Transmetallate with Cu(II): Redox Activity and Suppression of Detrimental Oxy-Myoglobin …

B Kaya, H Smith, Y Chen, MG Azad… - Inorganic …, 2024 - ACS Publications
The coordination chemistry and electrochemistry of novel N-acridine thiosemicarbazones
(NATs) were investigated along with their redox activity, antiproliferative efficacy …