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In search of better antibacterial and anticancer agents, a series of novel 4‐[3‐fluoro‐4‐(morpholin‐4‐yl)]phenyl‐1H‐1,2,3‐triazole derivatives were synthesized (6a‐l and 8a‐j) by using 3‐fluoro‐4‐morpholinoaniline, alkyne, and triflyl azide via an in situ generated 4‐(4‐azido‐2‐fluorophenyl)morpholine and evaluated for their antibacterial and anticancer activity in vitro. Antibacterial activity against three G+ bacterial strains and anticancer activity against breast cancer cell line (MCF‐7) and cervical carcinoma cell line (HeLa) was evaluated. Among all the tested compounds, 6h, 6i, and 8b exhibited potent antibacterial activity against tested gram‐positive bacterial strains. The anticancer activity screening results of 8f, 8h, and 8i exhibited potent cytotoxic activity against two cancer cell lines with IC50 values nearer to the standard drug, doxorubicin. The remaining compounds have shown good to moderate activity against the tested cell lines. On the basis of the results obtained, a structure‐activity relationship (SAR) is discussed.

The synthesis of some novel 4‐azaindole‐1,2,4‐oxadiazole hybrids (5 a–5 q) from the reaction between 1H‐pyrrolo[3,2‐b]pyridine‐3‐carbonitrile and readily available aromatic carboxylic acids using was described herein. All these hybrids were evaluated for their in vitro anticancer activity against three human cancer cell lines namely A375 (melanoma), MCF7 (breast) and A549 (lung) using MTT assay and outcomes revealed that three compounds like 5 c, 5 f and 5 m displayed superior inhibitory activities against all the cell lines than the standard. In those, predominantly, the compound 5 m showed outstanding activity in MCF‐7 cell line possessing IC50 values 0.48 μM. In addition, the in silico studies of three potent compounds 5 c, 5 f and 5 m were carried out to identify the interactions against EGFR receptor and found that the energy calculations were in good agreement with the obtained IC50 values. Furthermore, the compounds 5 c, 5 f and 5 m exhibited promising inhibitory activity against tyrosine kinase EGFR. Among them, the compounds 5 f and 5 m displayed superior activity against tyrosine kinase EGFR when compared with the standard Erlotinib.

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Cu/Pd catalyzed one pot synthesis of fused benzoxazino[1,2,3]triazolyl[4,5-c]quinolinone hybrids and their cytotoxic activity against human cancer cell lines MCF-7, HeLa and A-549 is described.