Impact of the New Hybrids of Glycoconjugate‐1,2,3‐triazole Tethered with 1,2,4‐oxadiazole as Promising Anticancer, Antimicrobial, and Antimalarial Agents

Abstract Click chemistry is adopted to synthesize the new hybrids of glycoconjugates‐1,2,3‐triazole tethered with 1,2,4‐oxadiazole 5a–c in a single step. Structure identification of the synthesized compounds was elucidated from their spectral analyses. The antiproliferative activity of the developed glycoconjugates was evaluated against MCF‐7 breast carcinoma, HeLa cervical carcinoma, and the normal Vero cell lines. Additionally, the antimicrobial and antimalarial potentials of the new glycoconjugates were estimated in vitro against a plethora of Gram‐negative and Gram‐positive bacteria, fungi, and Plasmodium chabaudi . The glycoconjugate 5b (benzyl substituted) exhibited 2.07‐fold more cytotoxic activity than doxorubicin against the MCF‐7 cell line. Regarding the HeLa cervical cell line, the glycoconjugate 5b (benzyl substituted) showed comparable potency to doxorubicin. Glycoconjugates 5a–c displayed significant inhibition against investigated bacterial and fungal strains. The glycoconjugate 5c (4‐trifluoromethylphenyl substituted) exhibited excellent antibacterial activity with 30.6 mm ZOI and MIC value of 1.95 µg/mL against Enterococcus faecalis and 29.8 mm ZOI and MIC value of 1.73 µg/mL against Staphylococcus aureus . The three glycoconjugates showed significant antimalarial activity. The glycoconjugate 5a (phenyl substituted) inhibited the parasite's growth by 94.6% at a concentration of 10 µg/mL, The results revealed the synthesized glycoconjugates as interesting therapeutic candidates for further development.

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Publication Details

Journal
ChemistrySelect
Published
2025-05-01
DOI
https://doi.org/10.1002/slct.202500187
Citations
2
Primary Topic
Click Chemistry and Applications
Type
article
Field-Weighted Citation Impact
1.87

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article

Impact of the New Hybrids of Glycoconjugate‐1,2,3‐triazole Tethered with 1,2,4‐oxadiazole as Promising Anticancer, Antimicrobial, and Antimalarial Agents

Laila F. Awad, Ibrahim Elghamry, Asmaa E. Kassab, Amr Negm et al.
2 citations
ChemistrySelect
Click Chemistry and Applications
1.87
article

Impact of the New Hybrids of Glycoconjugate‐1,2,3‐triazole Tethered with 1,2,4‐oxadiazole as Promising Anticancer, Antimicrobial, and Antimalarial Agents

Laila F. Awad, Ibrahim Elghamry, Asmaa E. Kassab, Amr Negm, Mohammed Salah Ayoup, Jawaher Y. Al Nawah
article en
2 citations

Abstract

Abstract Click chemistry is adopted to synthesize the new hybrids of glycoconjugates‐1,2,3‐triazole tethered with 1,2,4‐oxadiazole 5a–c in a single step. Structure identification of the synthesized compounds was elucidated from their spectral analyses. The antiproliferative activity of the developed glycoconjugates was evaluated against MCF‐7 breast carcinoma, HeLa cervical carcinoma, and the normal Vero cell lines. Additionally, the antimicrobial and antimalarial potentials of the new glycoconjugates were estimated in vitro against a plethora of Gram‐negative and Gram‐positive bacteria, fungi, and Plasmodium chabaudi . The glycoconjugate 5b (benzyl substituted) exhibited 2.07‐fold more cytotoxic activity than doxorubicin against the MCF‐7 cell line. Regarding the HeLa cervical cell line, the glycoconjugate 5b (benzyl substituted) showed comparable potency to doxorubicin. Glycoconjugates 5a–c displayed significant inhibition against investigated bacterial and fungal strains. The glycoconjugate 5c (4‐trifluoromethylphenyl substituted) exhibited excellent antibacterial activity with 30.6 mm ZOI and MIC value of 1.95 µg/mL against Enterococcus faecalis and 29.8 mm ZOI and MIC value of 1.73 µg/mL against Staphylococcus aureus . The three glycoconjugates showed significant antimalarial activity. The glycoconjugate 5a (phenyl substituted) inhibited the parasite's growth by 94.6% at a concentration of 10 µg/mL, The results revealed the synthesized glycoconjugates as interesting therapeutic candidates for further development.

ChemistrySelectVol. 10(17)
Cairo University (EG), King Faisal University (SA), Alexandria University (EG)
King Faisal University, Deanship of Scientific Research, King Saud University
Openalex Percentile: Top 16%
Click Chemistry and Applications
1.87
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