Ontology highlight
ABSTRACT:
SUBMITTER: Xu Q
PROVIDER: S-EPMC5150690 | biostudies-literature | 2016 Dec
REPOSITORIES: biostudies-literature
ACS medicinal chemistry letters 20161017 12
A series of 3,6-diaryl-[1,2,4]triazolo[4,3-<i>b</i>]pyridazines were designed as a class of vinylogous CA-4 analogues. The easily isomerized (<i>Z</i>,<i>E</i>)-butadiene linker of vinylogous CA-4 was replaced by a rigid [1,2,4]triazolo[4,3-<i>b</i>]pyridazine scaffold. Twenty-one target compounds were synthesized and exhibited moderate to potent antiproliferative activity. The compound <b>4q</b> with a 3-amino-4-methoxyphenyl moiety as the B-ring, comparable to CA-4 (IC<sub>50</sub> = 0.009-0.0 ...[more]