Synthesis, docking and anticancer evaluation of new pyridine-3-carbonitrile derivatives.
Eman Mansour; Ahmed A. Abd-Rabou; Ibrahim F. Nassar; Safaa.I.elewa;
Abstract
Nā-(2-((4-(Benzo[d][1, 3]dioxol-5-yl)-3-cyano-6-(naphthalen-2-yl)-pyridin-2-yl)oxy)-
acetyl)benzohydrazide (6) and hydrazide derivatives (7ā10) were synthesized
via reaction of 3-cyano-pyridinacetohydrazide (5) with benzoylchloride and
the appropriate aldehyde, respectively. Also, 4-(Benzo[d][1, 3]dioxol-5-yl)-2-(2-
(3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)-2-oxoethoxy)-6-(naphthalen-2-
yl) nicotinonitrile (11) was prepared through reaction of (5) with ethylace toacetate. In addition, the hydrazide 5 was used as a starting material for
synthesizing other nicotinonitrile derivatives (12, 13) and acetohydrazides
(14, 15). Moreover, new 2, 5-disubsitituted-1,3,4-oxadiazoles (16, 17) were
furnished by the reaction of (5) with benzoic acid derivatives. The cytotox icity for some new compounds was investigated against human breast
cancer MCF-7 and MDA-MB-231 cell lines at concentrations (0, 10, 20, 40,
60, 80, and 100 lg/ml) using MTT assay. Compounds (4, 9, 14 and 17)
were recorded the lowest half-maximal inhibitory concentrations (IC50s)
against MCF-7 and MDA-MB-231 cell lines via cytotoxicity assays. These
results were confirmed using molecular docking experiments. From the
previous observations, we suggested that our synthesized compounds
could be of great potential against breast cancer cells
acetyl)benzohydrazide (6) and hydrazide derivatives (7ā10) were synthesized
via reaction of 3-cyano-pyridinacetohydrazide (5) with benzoylchloride and
the appropriate aldehyde, respectively. Also, 4-(Benzo[d][1, 3]dioxol-5-yl)-2-(2-
(3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)-2-oxoethoxy)-6-(naphthalen-2-
yl) nicotinonitrile (11) was prepared through reaction of (5) with ethylace toacetate. In addition, the hydrazide 5 was used as a starting material for
synthesizing other nicotinonitrile derivatives (12, 13) and acetohydrazides
(14, 15). Moreover, new 2, 5-disubsitituted-1,3,4-oxadiazoles (16, 17) were
furnished by the reaction of (5) with benzoic acid derivatives. The cytotox icity for some new compounds was investigated against human breast
cancer MCF-7 and MDA-MB-231 cell lines at concentrations (0, 10, 20, 40,
60, 80, and 100 lg/ml) using MTT assay. Compounds (4, 9, 14 and 17)
were recorded the lowest half-maximal inhibitory concentrations (IC50s)
against MCF-7 and MDA-MB-231 cell lines via cytotoxicity assays. These
results were confirmed using molecular docking experiments. From the
previous observations, we suggested that our synthesized compounds
could be of great potential against breast cancer cells
Other data
Title | Synthesis, docking and anticancer evaluation of new pyridine-3-carbonitrile derivatives. | Authors | Eman Mansour; Ahmed A. Abd-Rabou; Ibrahim F. Nassar; Safaa.I.elewa | Keywords | KEYWORDS 3-Cyanopyridinacetohydrazide;1,3-Dioxole-5-carbaldehyde;1,3,4-Oxadiazoles;Cytotoxicity;Docking stud | Issue Date | 2021 | Publisher | taylor & francis | Journal | Polycyclic Aromatic Compounds |
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