Synthesis and Anticancer Activity of Novel 1,2,3-Triazole Ring
Incorporated 1,2,4-Oxadiazole-1,3-Oxazole Derivatives

Krishna, R. Jaya; Sridhar, Gattu; Jayaprakash, H. V.

doi:10.1134/s1070363220050242

Cited by 7 publications

(2 citation statements)

References 14 publications

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“…The electron-donating substituent on the phenyl ring attached to 1,2,3-triazole was the most active, and electronwithdrawing groups resulted in moderate activity of the compounds against all cell lines. [73] 2-Mercaptobenzimidazole-linked 1,2,3triazole hybrids 66 (IC 50 value of 18 μM) and 67 (IC 50 value of 20 μM) showed dose-dependent antiproliferative effects on C6 glioma, significantly increased early apoptosis, and acted as dual kinase and colchicine-binding site inhibitors. [74] Benzimidazole-1,2,3-triazole hybrid 68 has been reported as a G-quadruplex DNA groove binding molecule that shows anticancer activity on PCV3 and B16-F10 cancer cells and also induces both G 2 /M-phase arrest and apoptosis.…”

Section: 23-triazole-linked Azole Hybridsmentioning

confidence: 99%

1,2,3‐Triazole hybrids as anticancer agents: A review

Alam

2021

Archiv der Pharmazie

190

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Despite the advancements in the development of anticancer agents, more effective and safer anticancer drugs still need to be developed as the current agents cause unwanted side effects and many patients have become drug resistant. 1,2,3-Triazoles, due to their remarkable biological potential, have received considerable attention in drug discovery for the development of anticancer agents. The present review article presents an overview of the recent advances in 1,2,3-triazole hybrids with anticancer potential over the last 2 years, their chemical structures, structure-activity relationships, and mechanisms of action, as well as insights into the docking studies.

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Section: 23-triazole-linked Azole Hybridsmentioning

confidence: 99%

1,2,3‐Triazole hybrids as anticancer agents: A review

Alam

2021

Archiv der Pharmazie

190

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“…1,2,3‐Triazole‐1,2,4‐oxadiazole‐oxazole hybrids 22 (IC 50 : 0.14–13.3 µM, MTT assay) showed promising antiproliferative activity against MCF‐7 breast cancer cells, and the SAR elucidated that electron‐withdrawing group especially nitro group on the phenyl ring at the C‐4 position of 1,2,3‐triazole moiety was favorable to the activity. [ 43 ] Among them, hybrids 22a,b (IC 50 : 180 and 140 nM) were 11.7 and 15.0 times superior to etoposide (IC 50 : 2.11 µM) against MCF‐7 breast cancer cells. Hence, hybrids 22a,b could act as promising candidates for further evaluations.…”

Section: 23‐triazole‐azole Hybridsmentioning

confidence: 99%

The anti‐breast cancer therapeutic potential of 1,2,3‐triazole‐containing hybrids

Song,

Zhang,

Zhang

et al. 2023

Archiv der Pharmazie

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Breast cancer, as one of the most common invasive malignancies and the leading cause of cancer‐related deaths in women globally, poses a significant challenge in the world health system. Substantial advances in diagnosis and treatment have significantly improved the survival rate of breast cancer patients, but the number of incidences and deaths of breast cancer are projected to increase by 40% and 50%, respectively, by 2040. Chemotherapy is one of the principal treatments for breast cancer therapy, but multidrug resistance and severe side effects remain the major obstacles to the success of treatment. Hence, there is a vital need to develop novel chemotherapeutic agents to combat this deadly disease. 1,2,3‐Triazole, which can be effectively constructed by click chemistry, not only can serve as a linker to connect different anti‐breast cancer pharmacophores but also is a valuable pharmacophore with anti‐breast cancer potential and favorable properties such as hydrogen bonding, moderate dipole moment, and enhanced water solubility. Particularly, 1,2,3‐triazole‐containing hybrids have demonstrated promising in vitro and in vivo anti‐breast cancer potential against both drug‐sensitive and drug‐resistant forms and possessed excellent selectivity by targeting different biological pathways associated with breast cancer, representing privileged scaffolds for the discovery of novel anti‐breast cancer candidates. This review concentrates on the latest advancements of 1,2,3‐triazole‐containing hybrids with anti‐breast cancer potential, including work published between 2020 and the present. The structure–activity relationships (SARs) and mechanisms of action are also reviewed to shed light on the development of more effective and multitargeted candidates.

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