الفهرس 
IntroductionOnly 14 pages are availabe for public view
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Abstract
In this study, a novel series of indazole –based compounds was designed, synthesized and
biologically evaluated for its inhibitory activity against VEGFR-2 kinase enzyme. Three
compounds exhibited significantly high activity against the enzyme (XIIIb), (XIIIc) and (XIIIe),
showing IC50 values of 1.4, 1.3 and 8.1 nM respectively.
On the other side, fourteen compounds were selected by NCI, to be screened against their
panel of cancer cell lines for evaluation of their in vitro anticancer activity. Four compounds
(Ve, Vf, XIIIa and XIIIc) were further selected for five dose testing against NCI cancer cell lines;
as they displayed significant anticancer activity against NCI panel of cell lines. (Ve) exhibited
nanomolar GI50 values against CCRF-CEM (901 nM), MOLT-4 (525 nM) and CAKI-1 (992 nM)
and one digit micromolar activity against the rest of cell lines that ranged from 1.05 μM to 2.41
μM. Compound (Vf) had one digit micromolar activity against the whole panel of cell lines,
ranging from 1.55 ato 7.4 μM. Compound (XIIIa) displayed nanomolar activity against broad
spectrum of cell lines of different types where it exhibited its highest potency against T-47D
breast cancer cell line (GI50 = 183 nM). Additionally, it showed one digit micromolar GI50 on the
rest of cell lines panel ranging from1.01 to 5.22 μM. Compound (XIIIc)displayed nanomolar GI50
against two cell lines: KM12 colon cancer cell line (50 nM) and SF-539 CNS cancer cell line (612
nM), while it showed one digit micromolar GI50 on the rest of cell lines panel that ranged from
1.24 to 4.44 μM. However, the exact mechanism of cellular anticancer activity of these
compounds was not fully described but still a material for future investigation.