Abstract
Novel 6-aryl-2-methylnicotinic acid hydrazides
4a
-
c
and their corresponding hydrazones
5a
-
c
and
6a
-
i
were synthesized. X-ray single crystal diffraction of
6h
confirmed the chemical structure of hydrazones
6a-i
. Antiproliferative activity of the synthetic compounds was investigated against K562 leukemia cell lines. Variable cell growth inhibitory activities were obtained with IC
50
range from 24.99 to 66.78 μM where the compound
6c
exhibited the maximum activity. Structure activity relationship analysis has been performed and a common pharmacophore model for the synthesized derivatives has been obtained by using the pharmacophore elucidation module of the software MOE. The best model obtained is characterized by two projected locations of potential H-bond donors (F 3 and F4) and two Aromatic annotations (F1 and F2).