A new series of benzimidazole linked pyrazole derivatives were synthesized by cyclocondensation reaction through one-pot multicomponent reaction in absolute ethanol. All the synthesized compounds were tested for their in vitro anticancer activities on five human cancer cell lines including MCF-7, HaCaT, MDA-MB231, A549 and HepG2. EGFR receptor inhibitory activities were carried out for all the compounds. Majority of the compounds showed potent antiproliferative activity against the tested cancer cell lines. Compound 5a showed the most effective activity against the lungs cancer cell lines (IC₅₀ = 2.2 µM) and EGFR binding (IC₅₀ = 0.97 µM) affinity as compared to other members of the series. Compound 5a inhibited growth of A549 cancer cells by inducing a strong G₂/M phase arrest. In addition, same compound inhibited growth of A549 cancer cells by inducing apoptosis. In molecular docking studies compound 5a was bound to the active pocket of the EGFR (PDB 1M17) with five key hydrogen bonds and two π-π interaction with binding energies ΔG = −34.581 Kcal/mol.

通过在无水乙醇中的一锅多组分反应进行环缩合反应，合成了一系列新的苯并咪唑连接的吡唑衍生物。测试所有合成的化合物对包括MCF-7，HaCaT，MDA-MB231，A549和HepG2在内的5种人类癌细胞系的体外抗癌活性。对所有化合物都进行了EGFR受体抑制活性。大多数化合物对测试的癌细胞系显示出有效的抗增殖活性。与该系列的其他成员相比，化合物5a对肺癌细胞系（IC ₅₀ = 2.2 µM）和EGFR结合（IC ₅₀ = 0.97 µM）亲和力显示出最有效的活性。化合物5a诱导强G ₂ / M期阻滞抑制A549癌细胞的生长。此外，相同的化合物通过诱导细胞凋亡来抑制A549癌细胞的生长。在分子对接研究中，化合物5a通过五个关键氢键和两个π-π相互作用键合能ΔG= -34.581 Kcal / mol结合到EGFR（PDB 1M17）的活性口袋上。