Design, Synthesis, and Anticancer Activity of Novel 2-(4-Arylsubstituted-1H-1,2,3-triazol-1-yl)-N-{4-[2-(thiazol-2-yl)benzo[d]thiazol-6-yl]phenyl}acetamide Derivatives

Polothi, Ravikumar; Raolji, G. S. B.; Rao, Mandava V. Basaveswara; Sheelam, Kalidasu

doi:10.1134/s1070363220120452

Cited by 2 publications

(2 citation statements)

References 9 publications

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“…Replacement of the 4-methoxy group with an electron-withdrawing (4-nitro) group enhanced the anticancer activity. [63] Alraqa et al [64] reported benzotriazole fused-1,2,3-triazole hybrid 53, which showed 81-90.0% anticancer activity for A549 and H1299 lung cancer cell lines and good DNA binding constants in the range of 1.3 × 10 −3 to 11.90 × 10 −5 M −1 (Figure 6).…”

Section: 23-triazole-linked Azole Hybridsmentioning

confidence: 99%

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

Alam

2021

Archiv der Pharmazie

156

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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

156

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“…The 1,2,3‐triazole‐benzothiazole‐thiazole hybrids 9 (IC 50 : 0.10–20.5 µM, MTT assay) exhibited moderate to excellent antiproliferative activity against MCF‐7 breast cancer cells, and the SAR illustrated that hybrids with more electron‐donating groups or less electron‐withdrawing groups showed higher activity. [ 29 ] Among them, hybrids 9a,b (IC 50 : 100 and 120 nM) were 21.1 and 15.8 times superior to etoposide (IC 50 : 2.11 µM) against MCF‐7 breast cancer cells. Further studies revealed that the replacement of benzothiazole by benzimidazole was also tolerated, and hybrid 10 (IC 50 : 3.45 µM, MTT assay) was more potent than doxorubicin (IC 50 : >100 µM) against MCF‐7 breast cancer cells.…”

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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Design, Synthesis, and Anticancer Activity of Novel 2-(4-Arylsubstituted-1H-1,2,3-triazol-1-yl)-N-{4-[2-(thiazol-2-yl)benzo[d]thiazol-6-yl]phenyl}acetamide Derivatives

Cited by 2 publications

References 9 publications

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

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

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

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