Design, Synthesis, and Anticancer Activity of Drug-like Iron Chelators/G-Quadruplex Binders as Synergic Dual Targeting Agents.

Iron homeostasis is strictly related to numerous physiological pathways including cell cycle progression and cell growth. The newest anticancer strategies focus on either depleting the cells with a suitable chelator or increasing their loading by administering iron complexes to induce ferroptosis. Iron depletion inhibits cell proliferation, while iron overload induces the damage of guanine nucleobases in G-quadruplex structures via ROS generation, leading to genome instability.

Shielding siRNA by peptide-based nanofibers: An efficient approach for turning off EGFR gene in breast cancer.

Peptide-based self-assembled nanosystems show great promise as non-viral gene and siRNA delivery vectors. In the current study, we designed and functionalized nanofibers for the delivery of siRNA, targeting and silencing EGFR gene overexpressed in triple-negative breast cancer. The nanofiber-mediated siRNA delivery was characterized in terms of zeta potential, morphology, and structural stability by circular dichroism spectroscopy.

5-methyl-2-carboxamidepyrrole-based novel dual mPGES-1/sEH inhibitors as promising anticancer candidates.

Inhibiting microsomal prostaglandin E synthase-1 (mPGES-1), an inducible enzyme involved in prostaglandin E (PGE) biosynthesis and tumor microenvironment (TME) homeostasis, is a valuable strategy for treating inflammation and cancer. In this work, 5-methylcarboxamidepyrrole-based molecules were designed and synthesized as new compounds targeting mPGES-1. Remarkably, compounds 1f, 2b, 2c, and 2d were able to significantly reduce the activity of the isolated enzyme, showing IC values in the low micromolar range.

Chemical characterization of wheat-based waste derived from a pharmaceutical process for its potential valorization.

Introduction: We report the analysis and characterization and the preliminary biological evaluation, of both liquid and solid wastes obtained from the processing of wheat () to produce the most iconic phytostimulin-based pharmaceutical products. The study aims to verify whether the waste can be reused in another process and not destined to its simple destructive disposal.

Methods: In this perspective, we first carried out an in-depth chemical-physical analysis of the waste together with a biocompatibility evaluation to plan the feasible final choice of waste destination.

The combined use of biological investigations, bio chromatographic and in silico methods to solve the puzzle of badge and its derivative's toxicity.

Bisphenol A diglycidyl ether (BADGE) is a pre-polymer of BPA widely used in manufacturing of epoxy resins and plastics; due to its high reactivity, unintended by-products, such as chlorinated and hydrolysed products, can reach the human body. This research integrates multiple approaches such as computational predictions, chromatographic experiments, biological assays, and human biomonitoring studies to comprehensively evaluate the toxicological profiles of the parent compound and its derivatives. In silico predictions were first utilized to estimate the toxicological properties and interactions of BADGE derivatives, providing insights into their bioactivity.