作者:Vassiliki Giannouli、Nikolaos Lougiakis、Ioannis K. Kostakis、Nicole Pouli、Panagiotis Marakos、Alexios-Leandros Skaltsounis、Sangkil Nam、Richard Jove、David Horne、Roxane Tenta、Harris Pratsinis、Dimitris Kletsas
DOI:10.1016/j.bmcl.2016.09.056
日期:2016.11
A number of new 3,7-disubstituted pyrazolo[3,4-c]pyridines have been designed and synthesized from suitable 2-aminopyridines. The antiproliferative activity of the derivatives was determined against the pancreatic MIA PaCa-2 and ovarian SCOV3 cancer cell-lines. IC50 values of the most promising analogue 46 lie in the submicromolar or low micromolar range. Furthermore, compound 46 shows similar inhibitory
已经设计并由合适的2-氨基吡啶合成了许多新的3,7-二取代的吡唑并[3,4- c ]吡啶。确定了该衍生物对胰腺MIA PaCa-2和卵巢SCOV3癌细胞系的抗增殖活性。最有前途的类似物46的IC 50值在亚微摩尔或低微摩尔范围内。此外,化合物46显示出对DU145,A2058和PC-3癌细胞的相似抑制活性,阻断了G 0 / G 1期的细胞周期并诱导了凋亡,这由凋亡核的出现确定。