6 results match your criteria: "Al-Azhar University Cairo 11884 Egypt ametwaly@azhar.edu.eg.[Affiliation]"

Vascular endothelial growth factor receptor-2 (VEGFR-2) is a key regulator of tumor angiogenesis and has become an important target in anticancer drug development. In this study, novel nicotinamide-thiadiazol hybrids were synthesized and evaluated for their anti-breast cancer potential through VEGFR-2 inhibition. The compounds were assessed for their cytotoxicity against MDA-MB-231 and MCF-7 cell lines.

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A novel series of quinoxaline derivatives was designed and synthesized to target VEGFR-2, a receptor critical in cancer progression, with a focus on favorable pharmacophoric features. Among these derivatives, compound 11d emerged as a promising candidate, exhibiting potent cytotoxicity against MDA-MB-231 and MCF-7 cancer cell lines, with IC values of 21.68 μM and 35.

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Objective: This study aims to investigate the potential of designed 2,3-dihydro-1,3,4-thiadiazole derivatives as anti-proliferative agents targeting VEGFR-2, utilizing a multidimensional approach combining and analyses.

Methods: The synthesized derivatives were evaluated for their inhibitory effects on MCF-7 and HepG2 cancer cell lines. Additionally, VEGFR-2 inhibition was assessed.

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This work presents the synthesis and , and analyses of new thiadiazole derivatives that are designed to mimic the pharmacophoric characteristics of vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitors. A comprehensive evaluation of the inhibitory properties of the synthesized thiadiazole derivatives against the cancer cell lines MCF-7 and HepG2 identified several auspicious candidates. Among them, compound 14 showed remarkably low IC values of 0.

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In this work, new thieno[2,3-]pyrimidine-derived compounds possessing potential anticancer activities were designed and synthesized to target VEGFR-2. The thieno[2,3-]pyrimidine derivatives were tested for their abilities to inhibit VEGFR-2 and to prevent cancer cell growth in two types of cancer cells, MCF-7 and HepG2. Compound 18 exhibited the strongest anti-VEGFR-2 potential with an IC value of 0.

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Article Synopsis
  • - This research focused on developing new anticancer compounds based on theobromine to inhibit VEGFR-2 and tested their effectiveness against cancer cell lines MCF-7 and HepG2.
  • - The compound 15a showed the strongest anti-cancer properties, with low micromolar inhibitory concentrations (IC values of 0.76 μM for HepG2 and 1.08 μM for MCF-7) and significant apoptosis induction in HepG2 cells, increasing apoptosis rates substantially.
  • - Additionally, 15a demonstrated strong binding to VEGFR-2 and inhibited cell migration and wound healing in HepG2 cells, suggesting its potential as a new anticancer treatment based on both biological activity and
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