Novel heterocyclic analogues of bergenin as anti-mitotic agents: Design, synthesis, biological evaluation and molecular docking study

Rao, Banoth Venkateswara; Swain, Sonam; Siva, Bandi; Priya, Smriti; Jadav, Surender Singh; Jain, Nishant; Ramalingam, Vaikundamoorthy; Babu, K. Suresh

doi:10.1016/j.molstruc.2023.135048

Cited by 3 publications

(1 citation statement)

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“…1,2,3‐Triazole‐sugar hybrids 122a,b (IC 50 : 7.4 and 6.2 µM, MTT assay) were not inferior to nocodazole (IC 50 : 3.2 µM) against MCF‐7 breast cancer cells and displayed low cytotoxicity (IC 50 : 49 and 51 µM) toward normal HEK‐293T cells. [ 148 ] Mechanistically, the two hybrids arrested cells at the G2/M phase, increased expression of mitotic markers (Cyclin B1 and PLK1 proteins), generated oxidative stress and induced apoptosis.…”

Section: Miscellaneous 123‐triazole 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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Section: Miscellaneous 123‐triazole Hybridsmentioning

confidence: 99%