School of Chemistry and Biochemistry, Thapar University, Patiala 147004, India.
Bioorg Med Chem Lett. 2013 Jun 15;23(12):3667-72. doi: 10.1016/j.bmcl.2012.12.071. Epub 2013 Jan 4.
A series of novel coumarin-benzimidazole hybrids, 3-(1H-benzo[d]imidazol-2-yl)-7-(substituted amino)-2H-chromen-2-one derivatives of biological interest were synthesized. Six out of the newly synthesized compounds were screened for in vitro antitumor activity against preliminary 60 tumor cell lines panel assay. A significant inhibition for cancer cells was observed with compound 8 (more than 50% inhibition) compared with other compounds and active known drug 5-fluorouracil (in some cell lines) as positive control. Compound 8 displayed appreciable anticancer activities against leukemia, colon cancer and breast cancer cell lines.
一系列具有生物活性的新型香豆素-苯并咪唑杂合体，3-(1H-苯并[d]咪唑-2-基)-7-(取代氨基)-2H-色烯-2-酮衍生物被合成出来。新合成的化合物中有六种被筛选用于体外抗肿瘤活性，对初步的 60 个肿瘤细胞系进行了检测。与其他化合物和阳性对照活性已知药物 5-氟尿嘧啶（在某些细胞系中）相比，化合物 8 对癌细胞的抑制作用显著（超过 50%的抑制）。化合物 8 对白血病、结肠癌和乳腺癌细胞系表现出明显的抗癌活性。
