In:
Archiv der Pharmazie, Wiley, Vol. 346, No. 11 ( 2013-11), p. 840-850
Abstract:
A series of 4‐(2‐fluorophenoxy)‐2‐(1 H ‐tetrazol‐1‐yl)pyridines bearing semicarbazone moieties were synthesized and evaluated for their in vitro antitumor potency. Some of the compounds ( 10b , 10c , 10e – 10h , 10m – 10p , 10r , and 11b ) exhibited moderate to excellent antitumor activity as compared to sorafenib and PAC‐1, as well as low levels of toxicity toward the human fetal lung fibroblast cell line WI‐38. The most promising compound 10p (IC 50 = 0.08, 0.36, 0.97 µM) was 45.1‐, 6.1‐, and 2.4‐fold more active than sorafenib (IC 50 = 3.61, 2.19, 2.32 µM), and 17, 3.2, and 2.9 times better than PAC‐1 (IC 50 = 1.36, 1.17, 2.83 µM) against three cancer cell lines (HT‐29, H460, and MKN‐45), respectively. In addition, further studies examining enzymatic activity suggested that the marked pharmacological activity observed might be ascribed to an inhibitory action against CRAf kinase.
Type of Medium:
Online Resource
ISSN:
0365-6233
,
1521-4184
DOI:
10.1002/ardp.v346.11
DOI:
10.1002/ardp.201300188
Language:
English
Publisher:
Wiley
Publication Date:
2013
detail.hit.zdb_id:
1496815-0
SSG:
15,3
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