Vijay Avin B R, Thirusangu Prabhu, Lakshmi Ranganatha V, Firdouse Aiyesha, Prabhakar B T, Khanum Shaukath Ara
Molecular Biomedicine Laboratory, Postgraduate Department of Studies and Research in Biotechnology, Sahyadri Science College (Autonomous), Kuvempu University, Shimoga 577203, Karnataka, India.
Department of Chemistry, Yuvaraja's College (Autonomous), University of Mysore, Mysore 570 005, Karnataka, India.
Eur J Med Chem. 2014 Mar 21;75:211-21. doi: 10.1016/j.ejmech.2014.01.050. Epub 2014 Feb 2.
A sequence of coumarin analogs 5a-j was obtained by multi step synthesis from hydroxy benzophenones (1a-j). The in vitro antiproliferative effect of the title compounds was tested against Ehrlich ascites carcinoma (EAC) and Daltons lymphoma ascites (DLA) cell lines. Among the series, compound 5c with bromo group in the benzophenone moiety was endowed with excellent antiproliferative potency with significant IC50 value. Further, in vivo antitumor effect of compound 5c against murine EAC and solid DL tumor model system was evident by the extended survivality. The tumor inhibitory mechanism of compound 5c was due to the antiangiogenesis and promotion of apoptosis. These results suggest possible applications of compound 5c which could be developed as a potent anticancer drug in the near future.
通过多步合成从羟基二苯甲酮（1a-j）获得了一系列香豆素类似物5a-j。测试了标题化合物对艾氏腹水癌（EAC）和道尔顿淋巴瘤腹水（DLA）细胞系的体外抗增殖作用。在该系列中，二苯甲酮部分带有溴基团的化合物5c具有优异的抗增殖能力，IC50值显著。此外，化合物5c对小鼠EAC和实体DL肿瘤模型系统的体内抗肿瘤作用通过延长生存期得以体现。化合物5c的肿瘤抑制机制是由于抗血管生成和促进细胞凋亡。这些结果表明化合物5c可能具有应用前景，有望在不久的将来开发成为一种有效的抗癌药物。
