In the designed compounds, either a biarylamide or biarylurea moiety or an N-substituted piperazine motif was linked to position 1 of the phthalazine core. The anti-proliferative activity of the synthesised compounds revealed that eight compounds (
6b, 6e, 7b, 13a, 13c, 16a, 16d and 17a
) exhibited excellent broad spectrum cytotoxic activity in NCI 5-log dose assays against the full 60 cell panel with GI
50
values ranging from 0.15 to 8.41 µM. Moreover, the enzymatic assessment of the synthesised compounds against VEGFR-2 tyrosine kinase showed the significant inhibitory activities of the biarylureas (
12b, 12c and 13c
) with IC
50
s of 4.4, 2.7 and 2.5 μM, respectively, and with 79.83, 72.58 and 71.6% inhibition of HUVEC at 10 μM, respectively. Additionally, compounds (
7b, 13c and 16a)
were found to induce cell cycle arrest at S phase boundary. Compound
7b
triggered a concurrent increase in cleaved caspase-3 expression level, indicating the apoptotic-induced cell death.
Phytochemical investigation of Premna odorata Blanco “Lamiaceae” young stems afforded four new acylated rhamnopyranoses 1–4, along with fourteen known compounds 5–19.
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