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Pharmaceuticals, Volume 10, Issue 3 (September 2017) – 19 articles
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Cover Story (view full-size image) The consolidation of the combretastatin and bisindolylmaleimide templates towards the inclusion of [...] Read more. The consolidation of the combretastatin and bisindolylmaleimide templates towards the inclusion of a novel heterocyclic ring has identified a novel indole trimethoxyphenyl aminopyrazole as an anticancer lead. The unique electronic nature of the 5-aminopyrazole moiety allows for regiospecific substitution on different sites of the ring and further expansion to pyrazolotriazinedione and pyrazolopyrimidine bicyclic systems is possible. The antiproliferative activities of the 3,4-diaryl-5-aminopyrazoles were assessed using the NCI-60 cell screen, disclosing the discovery of distinct selectivity profiles towards a number of cell lines. The lead compound 55 is effective at reducing the growth of HOP-92 lung cancer, UO-31 and CAKI-1 renal cancer cells below 20%. View the paper here