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<p>Newly synthesized compounds 7, 8, and 9 and their nanogels as nano-carrier drug delivery systems have been synthesized and estimated for their cytotoxicity on MCF-7, HCT-116, HepG2, and A549. This research emphasizes on the formation and description of the Cs/PVA nanogel loaded with our derivatives <b>7</b>, <b>8,</b> and <b>9</b>. The stability of nanogel formation was elucidated by zeta potential values which remained negative with values of -6.8, -11.8, and -7.8&#xa0;mV respectively. The obtained compounds and their nanogels were evaluated as Topo-II inhibitors and DNA intercalators. The nanogel for compound <b>7</b> enhanced cytotoxicity in A549, HCT116, MCF-7, and HepG2 cancers by 35.93%, 34.29%, 50.91%, and 49.94% respectively. Moreover, the nanogel for compound <b>8</b> enhanced cytotoxicity in A549, HCT116, MCF-7, and HepG2 cancers by 31.13%, 34.09%, 49.59%, and 46.43% respectively. Furthermore, the nanogel for compound <b>9</b> enhanced cytotoxicity in A549, HCT116, MCF-7, and HepG2 cancers by 38.99%, 43.78%, 58.25%, and 57.73% respectively. Moreover, our derivatives <b>7</b>, <b>7 (nanogel)</b>, <b>8, 8 (nanogel)</b>, <b>9</b> and <b>9 (nanogel)</b> exhibited high selectivity against cancer cells and lower toxicity on VERO cells with IC<sub>50</sub> = 45.90–49.90&#xa0;μM. Furthermore, the new derivatives demonstrated in silico very good anticipated ADMET profile. The nano-carrier formulations for the new derivatives may be purposeful as a prototype for future design, optimization, adaptation and investigation to obtain farther powerful selective anticancer agents.</p>

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Nano-carrier, design, synthesis, in silico ADMET, anti-proliferative assessments and docking of [1,2,4]triazolo[4,3-a]quinoxalines as Topo-II inhibitors and DNA intercalators

  • 期刊论文

  • 发表日期：

    2025年4月11日

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  • Ahmed K. B. Aljohani,
  • Sara A. Almadani,
  • Marwa Alsulaimany,
  • Naif Aljuhani,
  • Waad A. Samman,
  • Adel H. Al-Shareef,
  • Read Alghamdi,
  • Saeed M. Tayeb,
  • Hussam Y. Alharbi,
  • Majed S. Aljohani,
  • Khaled El‐Adl,
  • Mo’men Salem

摘要

Newly synthesized compounds 7, 8, and 9 and their nanogels as nano-carrier drug delivery systems have been synthesized and estimated for their cytotoxicity on MCF-7, HCT-116, HepG2, and A549. This research emphasizes on the formation and description of the Cs/PVA nanogel loaded with our derivatives 7, 8, and 9. The stability of nanogel formation was elucidated by zeta potential values which remained negative with values of -6.8, -11.8, and -7.8 mV respectively. The obtained compounds and their nanogels were evaluated as Topo-II inhibitors and DNA intercalators. The nanogel for compound 7 enhanced cytotoxicity in A549, HCT116, MCF-7, and HepG2 cancers by 35.93%, 34.29%, 50.91%, and 49.94% respectively. Moreover, the nanogel for compound 8 enhanced cytotoxicity in A549, HCT116, MCF-7, and HepG2 cancers by 31.13%, 34.09%, 49.59%, and 46.43% respectively. Furthermore, the nanogel for compound 9 enhanced cytotoxicity in A549, HCT116, MCF-7, and HepG2 cancers by 38.99%, 43.78%, 58.25%, and 57.73% respectively. Moreover, our derivatives 7, 7 (nanogel), 8, 8 (nanogel), 9 and 9 (nanogel) exhibited high selectivity against cancer cells and lower toxicity on VERO cells with IC50 = 45.90–49.90 μM. Furthermore, the new derivatives demonstrated in silico very good anticipated ADMET profile. The nano-carrier formulations for the new derivatives may be purposeful as a prototype for future design, optimization, adaptation and investigation to obtain farther powerful selective anticancer agents.