Natural Products Chemistry Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, Andhra Pradesh, India.
Eur J Med Chem. 2013 Jul;65:389-402. doi: 10.1016/j.ejmech.2013.03.042. Epub 2013 Apr 18.
2-Oxo-2H-chromenylpyrazolecarboxylates (8a-h and 12a-zb) have been synthesized by [3 + 2] cycloaddition of 2H-chromenophenylhydrazones (7a-h and 11a-w) with diethyl/dimethylbut-2-ynedioates. Phenylchromeno[4,3-c]pyrazol-4(1H)-ones (13i-n) were prepared from corresponding phenylhydrazones (7a-h) with catalytic amount of piperidine in presence of pyridine as a solvent at 100 °C. All the synthesized compounds (8a-h, 12a-zb and 13a-n) were screened for anticancer activity against three human cancer cell lines such as prostate (DU-145), lung adenocarcinoma (A549), and cervical (HeLa) by standard MTT assay method. Further, photophysical properties (UV and fluorescence) for these compounds were discussed.
2-氧代-2H-色烯基吡唑羧酸酯（8a-h 和 12a-zb）是通过 2H-色烯基苯腙（7a-h 和 11a-w）与二乙基/二甲基丁-2-炔二酸酯的[3+2]环加成反应合成的。苯并色烯并[4,3-c]吡唑-4(1H)-酮（13i-n）是由相应的苯腙（7a-h）在吡啶作为溶剂的条件下，用催化量的哌啶在 100°C 下制备的。所有合成的化合物（8a-h、12a-zb 和 13a-n）都通过标准的 MTT 测定法对三种人类癌细胞系（前列腺（DU-145）、肺腺癌（A549）和宫颈（HeLa））进行了抗癌活性筛选。此外，还讨论了这些化合物的光物理性质（紫外和荧光）。
