摘要已发现,水合四丁基氟化铵比无水盐能更有效地将邻位和金属closo-carborane衍生物R'R''C 2 B 10 H 10转化为Nido-carborane阴离子[R' R” C 2 B 9 H 10]-,允许使用其他脱硼试剂难以制备或难以获得的许多新的Nido-carborane衍生物,特别是间-carborane衍生物[7,9-R'R“ -7,9-C 2 B 9 H 10]-[Bu 4 N] +(R'= 4-HOC 6 H 4,4-O 2 NC 6 H 4; R''= H且R'= R''= 4-PhOC 6 H 4,4-O 2 NC 6 H 4,2-C 5 H 4 N,4-H 2 NC 6 H 4)。用双(对-溴苯基-邻-甲碳烷基)苯1,4- [4-BrC 6 H 4 CB 10 H 10 C] 2 C 6 H 4进行实验,以确定脱硼所需的氟化四丁基铵的量两个笼子都放了盐1
Synthesis and biological evaluation of meta-carborane-containing phenoxyacetanilides as inhibitors of hypoxia-inducible factor (HIF)-1 transcriptional activity
摘要:
meta-Carboranylphenoxyacetanilides were synthesized by copper catalyzed coupling reaction of meta-carborane and phenyl iodides. The synthesized compounds were evaluated for their ability to inhibit hypoxia-induced HIF-1 transcriptional activity using a cell-based reporter gene assay. Among the compounds synthesized, meta-carborane containing phenoxyanilides 2d and 2h, which have an isobutyl group on meta-carborane, exhibited significant inhibition of hypoxia-induced HIF-1 transcriptional activity toward HeLa cell-based reporter gene assay with the IC50 values of 0.73 and 0.55 mu M, respectively. (C) 2015 Elsevier B.V. All rights reserved.