Dual-emissive ratiometric "turn-on" probe for real-time sensing of HSO in environmental samples and live cells.

The optical detection of hydrogen sulfate anion (HSO) in the aqueous phase is particularly challenging and relatively rare, mainly due to their extremely high Gibbs free energy of hydration, which stabilizes the ions and hinders their interaction with the sensors. A novel ratiometric "turn-on" fluorometric probe, N-hydroxy-6-((2-(4-methoxyphenyl)quinolin-6-yl)oxy)hexanamide (5C), was rationally designed and synthesized to enable highly selective and ultrasensitive detection of hydrogen sulfate ion (HSO) in aqueous phase. The probe 5C exhibits bathochromic shift of 52 nm in its emission spectrum upon HSO addition, resulting into fluorometric color change from non-fluorescent to a strong blue fluorescence under UV light.

A systematic review of the effects of nanoplastics on fish.

The global concern about plastics has been amplified due to their widespread contamination in the environment and their ability to cross biological barriers in living organisms. However, our understanding of their bioaccumulation, toxicity, and interaction with other environmental pollutants remains limited. Plastics are classified into three categories: macro-(MAP > 5 mm), micro-(MIP, <5 mm), and nanoplastics (NAP≤ 100 nm).

Design and Synthesis of Topoisomerases-Histone Deacetylase Dual Targeted Quinoline-Bridged Hydroxamates as Anticancer Agents.

The multifactorial nature of cancer requires treatment that involves simultaneous targeting of associated overexpressed proteins and cell signaling pathways, possibly leading to synergistic effects. Herein, we present a systematic study that involves the simultaneous inhibition of human topoisomerases (hTopos) and histone deacetylases (HDACs) by multitargeted quinoline-bridged hydroxamic acid derivatives. These compounds were rationally designed considering pharmacophoric features and catalytic sites of the cross-talk proteins, synthesized, and assessed for their anticancer potential.

A systematic review of the toxic potential of parabens in fish.

Parabens are the most prevalent ingredients in cosmetics and personal care products (PCPs). They are colorless and tasteless and exhibit good stability when combined with other components. Because of these unique physicochemical properties, they are extensively used as antimicrobial and antifungal agents.

Design, synthesis, and anticancer assessment of structural analogues of ()-1-((3,4,5-trimethoxybenzylidene)amino)-4-(3,4,5-trimethoxyphenyl)imidazo[1,2-]quinoxaline-2-carbonitrile (6b), an imidazo[1,2-]quinoxaline-based non-covalent EGFR inhibitor.

In our quest to find improved anticancer therapeutics, we expedite the lead optimization of ()-1-((3,4,5-trimethoxybenzylidene)amino)-4-(3,4,5-trimethoxyphenyl)imidazo[1,2-]quinoxaline-2-carbonitrile (6b), an EGFR inhibitor previously discovered in our laboratory through an in-house screening program. The lead optimization was rationally initiated considering the catalytic site of EGFR. We synthesized twenty-nine new analogues of 6b and assessed their anticancer activities.

Targeting the Epidermal Growth Factor Receptor with Molecular Degraders: State-of-the-Art and Future Opportunities.

Epidermal growth factor receptor (EGFR) is an oncogenic drug target and plays a critical role in several cellular functions including cancer cell growth, survival, proliferation, differentiation, and motility. Several small-molecule tyrosine kinase inhibitors (TKIs) and monoclonal antibodies (mAbs) have been approved for targeting intracellular and extracellular domains of EGFR, respectively. However, cancer heterogeneity, mutations in the catalytic domain of EGFR, and persistent drug resistance limited their use.

In Vivo Anticancer Evaluation of 6b, a Non-Covalent Imidazo[1,2-]quinoxaline-Based Epidermal Growth Factor Receptor Inhibitor against Human Xenograft Tumor in Nude Mice.

Tyrosine kinase inhibitors are validated therapeutic agents against EGFR-mutated non-small cell lung cancer (NSCLC). However, the associated critical side effects of these agents are inevitable, demanding more specific and efficient targeting agents. Recently, we have developed and reported a non-covalent imidazo[1,2-]quinoxaline-based EGFR inhibitor (), which showed promising inhibitory activity against the gefitinib-resistant H1975(L858R/T790M) lung cancer cell line.

Epidermal Growth Factor Receptor and its Trafficking Regulation by Acetylation: Implication in Resistance and Exploring the Newer Therapeutic Avenues in Cancer.

Background: The EGFR is overexpressed in numerous cancers. So, it becomes one of the most favorable drug targets. Single-acting EGFR inhibitors on prolong use induce resistance and side effects.