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Novel Diselenide Bis-Schiff bases tagged with diphenyl ethers: Promising candidates for selective treatment of hypopharyngeal and breast adenocarcinoma.

Bioorg Chem

August 2025

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Horus University-Egypt, New Damietta 34518, Egypt.; Department of Pharmaceutical Chemistry, College of Pharmacy, The University of Mashreq, Baghdad 10023, Iraq.. Electronic address:

Organoselenium (OSe) compounds have received much attention due to their potential to inhibit tumor growth while also protecting cells from oxidative damage, making them promising cancer prevention agents. However, diphenyl diselenide (PhSe) has many drawbacks, such as increased lipophilicity with low oral bioavailability, toxicity issues due to poor selectivity, and limited physicochemical criteria. In this study, we developed two novel sets of diphenyl ether 5a-g and diphenyl ether hybridized with diselenide 6a-g and evaluated their anticancer activity and underlying cytotoxic mechanisms.

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In connection with previous work on V-shaped polycyclic thiazolo[5,4-]quinazolin-9-one and [5,4-]quinazoline derivatives that can modulate the activity of various kinases, the synthesis of straight thiazole-fused [4,5-] or [5,4-]quinazolin-8-ones and quinazoline derivatives hitherto undescribed was envisioned. An innovative protocol allowed to obtain the target structures. The synthesis of inverted thiazolo[4,5-] and [5,4-]quinazolin-8-one derivatives was also explored with the aim of comparing biological results.

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Breast and colorectal cancers are the most common tumors, with high recurrence and low survival rates. We designed and synthesized a series of spirooxindole pyrrolidinyl derivatives, which were further evaluated for anti-proliferative activity using MDA-MB-468 and HCT 15 cell lines. The best inhibitor of this class, compound 6f, showed a very good inhibition potency, both on the MDA-MB-468 and HCT 15 cells as confirmed by molecular docking and molecular dynamic studies that predicted its binding mode into the active site of the targets.

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Anticancer Properties Against Select Cancer Cell Lines and Metabolomics Analysis of Tender Coconut Water.

Anticancer Agents Med Chem

April 2025

Dr. Hiram C. Polk, Jr., MD, Department of Surgery, and Price Institute of Surgical Research, School of Medicine, University of Louisville, Louisville, KY, 40202, United States.

Background: Tender Coconut Water (TCW) is a nutrient-rich dietary supplement that contains bioactive secondary metabolites and phytohormones with anti-oxidative and anti-inflammatory properties. Studies on TCW's anti-cancer properties are limited and the mechanism of its anti-cancer effects have not been defined.

Objective: In the present study, we investigate TCW for its anti-cancer properties and, using untargeted metabolomics, we identify components form TCW with potential anti-cancer activity.

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Natural products contribute substantially to anticancer therapy; the plant kingdom provides an important source of molecules. Conofolidine is a novel bisindole alkaloid isolated from the Malayan plant . Herein, we report conofolidine's broad-spectrum anticancer activity together with that of three other bisindoles-conophylline, leucophyllidine, and bipleiophylline-against human-derived breast, colorectal, pancreatic, and lung carcinoma cell lines.

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