Antiproliferative Activity of Some Newly Synthesized Substituted Pyridine Candidates Using 4‑(Aaryl)-6-(naphthalen-1-yl)-2-oxo-1,2- dihydropyridine-3-carbonitrile as Synthon
El-Hag, Amira; Elsayed A. Elsayed; Abd El-Galil E. Amr;
Abstract
Herein, we used nicotinonitrile derivatives 4a,b as scaffolds to build novel and active antineoplastic agents. The
reaction of nicotinonitrile derivatives 4a,b with POCl3/PCl5 and/or hydrazine hydrate afforded 2-chloropyridones 6a,b and 2-
hydrazinyl nicotinonitrile derivatives 11a,b, respectively, as building blocks for various heterocyclic compounds. The structures of all
of the synthesized heterocycles were elucidated from their spectral and elemental analyses. The cytotoxic activities of the prepared
derivatives were evaluated against different cancer cell lines. Results revealed potential cytotoxic effects of the synthesized
compounds against evaluated cell lines, where NCIH 460 and RKOP 27 cell lines were the most affected by the prepared
compounds. Derivative 14a was the most effective against all tested cell lines in terms of the obtained IC50 values (25 ± 2.6, 16 ± 2,
127 ± 25, 422 ± 26, and 255 ± 2 nM against NCIH 460, RKOP 27, HeLa, U937, and SKMEL 28 cells, respectively).
reaction of nicotinonitrile derivatives 4a,b with POCl3/PCl5 and/or hydrazine hydrate afforded 2-chloropyridones 6a,b and 2-
hydrazinyl nicotinonitrile derivatives 11a,b, respectively, as building blocks for various heterocyclic compounds. The structures of all
of the synthesized heterocycles were elucidated from their spectral and elemental analyses. The cytotoxic activities of the prepared
derivatives were evaluated against different cancer cell lines. Results revealed potential cytotoxic effects of the synthesized
compounds against evaluated cell lines, where NCIH 460 and RKOP 27 cell lines were the most affected by the prepared
compounds. Derivative 14a was the most effective against all tested cell lines in terms of the obtained IC50 values (25 ± 2.6, 16 ± 2,
127 ± 25, 422 ± 26, and 255 ± 2 nM against NCIH 460, RKOP 27, HeLa, U937, and SKMEL 28 cells, respectively).
Other data
Title | Antiproliferative Activity of Some Newly Synthesized Substituted Pyridine Candidates Using 4‑(Aaryl)-6-(naphthalen-1-yl)-2-oxo-1,2- dihydropyridine-3-carbonitrile as Synthon | Authors | El-Hag, Amira ; Elsayed A. Elsayed; Abd El-Galil E. Amr | Issue Date | 19-Feb-2021 | Publisher | American Chemical Society | Journal | ACS Omega | Volume | 6 | Start page | 7147 | End page | 7156 | DOI | https://dx.doi.org/10.1021/acsomega.1c00202 |
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