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 …

NDRG1 acts as an oncogene in triple-negative breast cancer and its loss sensitizes cells to mitochondrial iron chelation

SB Jadhav, M Vondrackova, P Potomova… - Frontiers in …, 2024 - frontiersin.org
Multiple studies indicate that iron chelators enhance their anti-cancer properties by inducing
NDRG1, a known tumor and metastasis suppressor. However, the exact role of NDRG1 …

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 …

[HTML][HTML] Multi-modal mechanisms of the metastasis suppressor, NDRG1: Inhibition of WNT/β-catenin signaling by stabilization of protein kinase Cα

MG Azad, M Hussaini, TM Russell, V Richardson… - Journal of Biological …, 2024 - Elsevier
The metastasis suppressor, N-myc downstream regulated gene-1 (NDRG1), inhibits pro-
oncogenic signaling in pancreatic cancer (PC). This investigation dissected a novel …