A new bunch of substituted aryl amino derivatives structurally modified pyrido3,2-dpyrimidines (10a-j) have been synthesized and evaluated for anticancer effects against PC3 (human prostate), A549 ...(human lung), MCF-7 (human breast) and Colo-205 (human colon) cancer cell lines by utilizing of MTT procedure. Most of the synthesized compounds were showed anticancer activity good to moderate activities with IC
50
values range from 0.013 ± 0.0058 µM to 8.22 ± 5.87 µM, whereas, standard 9 etoposide used as standard drug) showed IC
50
values from 0.14 ± 0.017 µM to 3.08 ± 0.135 µM, respectively. Among the synthesized compounds, five compounds 10a, 10b, 10c, 10d and 10e demonstrated more potent activity on all cell lines. Mainly, compound 10e displayed higher anticancer activity.
In this paper, we describe the synthesis of some new quinoxaline‐piperazine‐oxazole amide conjugates 6a‐n from 3‐chloroquinoxaline‐2‐carbonitrile using well‐known reaction sequences. The synthesized ...compounds were characterized by 1H NMR,13C NMR, and mass spectral analysis. The compounds were tested for their in vitro antiproliferative activity toward four different cancer cell lines such as PC‐3, MCF‐7, DU‐145, and A‐549 by MTT method. The compounds, 6c, 6h, 6i, and 6n were found to be more potent than the standard Erlotinib. In vitro tyrosine kinase EGFR inhibition studies using four potent compounds revealed that 6n has double inhibiting tendency with value IC50 of 0.22 μM and 6h with value of IC50 0.27 μM compared to reference compound. Molecular docking studies of active compounds, 6c, 6h, 6i, and 6n on EGFR receptor suggested that all the compounds have more binding energies than that of Erlotinib. Furthermore, the in silico pharmacokinetic profile was accomplished for the active compounds, 6c, 6h, 6i, and 6n using SWISS/ADME and pk CSM, whereas compounds, 6h, 6i, and 6c followed Lipinski rule, Veber rule, Egan rule and Muegge rule. The remaining compound 6n did not follow Lipinski rule, Ghose rule because one common violation, that is, because of high molecular weight (MW > 350).
Herein, we described the synthesis of some new phthalazine piperazine‐pyrazole conjugates(6a‐n) and their in vitro anticancer activity against four human cancer cell lines such as PC‐3, MCF‐7, DU‐145, and A‐549. The anticancer activity results reveals that the four compounds 6c, 6h, 6i, and 6n shown promising activity than the standard drug Erlotinib. Furthermore, the in silico studies of compounds 6c, 6h, 6i, and 6n supports the in vitro anticancer results. In addition, ADMET analyses were carried out on four potent compounds and results accordant with the in vitro anticancer and in vitro EGFR tyrosine kinase inhibition data.
A unique library of amide functionality carrying bis-1,3,4-oxadiazole-oxazolo4,5-bpyridin-2-yl) derivatives (10a-j) with proven chemical structures has been synthesised. They were tested for ...preliminary anticancer properties against various human cancer cell lines such as human prostate cancer (PC3), human lung cancer (A549), human breast cancer (MCF-7) and human colon cancer (Colo-205) using the MTT assay and chemotherapeutic agents such as etoposide as the reference drug. When compared to etoposide, all drugs shown greater efficacy against all cell lines.
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