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A series of novel theophylline-7-acetic acid (acefylline)-derived 1,2,4-triazole hybrids with N -phenyl acetamide moieties ( 11a - j ) have been synthesized and tested for their inhibitory ( in vitro ) potential against two cancer cell lines, A549 (lung) and MCF-7 (breast), using MTT assay. Among these derivatives, 11a , 11c , 11d , 11g , and 11h displayed remarkable activity against both cancer cell lines having cell viability values in the 21.74 ± 1.60-55.37 ± 4.60% range compared to acefylline (86.32 ± 1.75%) using 100 μg/μL concentration of compounds. These compounds were further screened against the A549 cancer cell line (lung) to find their half-maximal inhibitory concentration (IC 50 ) by applying various concentrations of these compounds. Compound 11g (2-(5-((1,3-dimethyl-2,6-dioxo-2,3-dihydro-1 H -purin-7(6 H )-yl)methyl)-4-phenyl-4 H -1,2,4-triazol-3-ylthio)- N - p -tolylacetamide) with the least IC 50 value (1.25 ± 1.36 μM) was discerned as a strong inhibitor of cancer cell multiplication in both cell lines (A549 and MCF-7). Their hemolytic studies revealed that all of them had very low cytotoxicity. Finally, in silico modeling was carried out to find the mode of binding of the highly active compound ( 11g ), which was according to the results of anti-cancer activity.

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Synthesis, Hemolytic Studies, and <i>In Silico</i> Modeling of Novel Acefylline–1,2,4-Triazole Hybrids as Potential Anti-cancer Agents against MCF-7 and A549

Synthesis, Hemolytic Studies, and In Silico Modeling of Novel Acefylline–1,2,4-Triazole Hybrids as Potential Anti-cancer Agents against MCF-7 and A549