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<p>A series of L-<i>tert</i>-leucine derivatives were designed, synthesized, characterized, and evaluated for cytotoxic activities, viz. MTT assayapoptosis-induction effects, cell-cycle analysis, EGFR-TK inhibition activity, and molecular docking studies. Twelve derivatives were synthesized and characterized by spectral data. The cytotoxic potential of the compounds was evaluated by MTT assay, against four cancerous cell lines (MCF-7, SKOV3, DU145, and A549), and one nontumorigenic cell line (HEK). The results obtained by MTT assay, indicated that compound <b>3d</b> was most potent among those synthesized, with IC<sub>50</sub> values 8.69 and 10.54 μM against DU145 cell lines and SKOV3 cell lines. Results were compared with the positive control, doxorubicin. Cell-cycle analysis and apoptosis suggested that <b>3d</b> displayed good antiproliferative activity by arresting the Sub G0 phase in the cell cycle and induced early and late apoptosis in cancer cells. Docking studies and EGFR-TK inhibition assay proposed that <b>3d</b> had good binding affinity toward the EGFR enzyme and acts as its potential inhibitor (IC<sub>50</sub> 0.517 μM). Based on the above findings, it is therefore concluded that L-<i>tert</i>-leucine derivatives can be considered as potential leads for cancer targets.</p>

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Design, Synthesis, Evaluation and Molecular Docking Studies of L-Tert-Leucine Derivatives for Cytotoxic Activities

  • 期刊论文

  • 发表日期：

    2025年2月1日

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  • Mahalakshmi C. S. Parepalli,
  • Rajitha Galla

摘要

A series of L-tert-leucine derivatives were designed, synthesized, characterized, and evaluated for cytotoxic activities, viz. MTT assayapoptosis-induction effects, cell-cycle analysis, EGFR-TK inhibition activity, and molecular docking studies. Twelve derivatives were synthesized and characterized by spectral data. The cytotoxic potential of the compounds was evaluated by MTT assay, against four cancerous cell lines (MCF-7, SKOV3, DU145, and A549), and one nontumorigenic cell line (HEK). The results obtained by MTT assay, indicated that compound 3d was most potent among those synthesized, with IC50 values 8.69 and 10.54 μM against DU145 cell lines and SKOV3 cell lines. Results were compared with the positive control, doxorubicin. Cell-cycle analysis and apoptosis suggested that 3d displayed good antiproliferative activity by arresting the Sub G0 phase in the cell cycle and induced early and late apoptosis in cancer cells. Docking studies and EGFR-TK inhibition assay proposed that 3d had good binding affinity toward the EGFR enzyme and acts as its potential inhibitor (IC50 0.517 μM). Based on the above findings, it is therefore concluded that L-tert-leucine derivatives can be considered as potential leads for cancer targets.