Synthesis of New 1,3,5-Triazine-Based 2-Pyrazolines as Potential Anticancer Agents

Moreno, Leydi M.; Quiroga, Jairo; Abonı́a, Rodrigo; Ramírez-Prada, Jonathan; Insuasty, Braulio

doi:10.3390/molecules23081956

Cited by 50 publications

(26 citation statements)

References 39 publications

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“…Moreno et al [75] reported the synthesis of some novel series of The presence of halogen atoms (Cl and F) in most cases increases the activity. [75] Singla et al [76] synthesized novel series of 1,3,5-triazinebenzimidazole analogs and investigated them for their in vitro anticancer activities.…”

Section: Anticancer Agentsmentioning

confidence: 99%

1,3,5‐Triazine: A versatile pharmacophore with diverse biological activities

Singh

Mandal

Masih

et al. 2021

Archiv der Pharmazie

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1,3,5-Triazine and its derivatives have been the epicenter of chemotherapeutic molecules due to their effective biological activities, such as antibacterial, fungicidal, antimalarial, anticancer, antiviral, antimicrobial, anti-inflammatory, antiamoebic, and antitubercular activities. The present review represents a summarized report of the crucial biological activities possessed by substituted 1,3,5-triazine derivatives, with special attention to the most potent compounds.

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Section: Anticancer Agentsmentioning

confidence: 99%

1,3,5‐Triazine: A versatile pharmacophore with diverse biological activities

Singh

Mandal

Masih

et al. 2021

Archiv der Pharmazie

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“…More recently, Insuasty et al reported the synthesis and evaluation of a series of chalcone derived 1,3,5-triazine containing 2-pyrazolines. Seventeen of them were selected and screened by NCI, where compounds 72 – 74 ( Figure 25 ) were proved to be the most potent of the library, along with the chalcone precursor of 74 [ 156 ]. The lowest GI 50 value was determined for 72 against renal cell line RXF-393 (0.569 μM) and breast HS-578 (0.644 μM).…”

Section: 2-pyrazolinesmentioning

confidence: 99%

Pyrazoline Hybrids as Promising Anticancer Agents: An Up-to-Date Overview

Matiadis

Sagnou

2020

IJMS

104

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Pyrazolines are five-membered heterocycles possessing two adjacent nitrogens. They have attracted significant attention from organic and medicinal chemists due to their potent biological activities and the numerous possibilities for structural diversification. In the last decade, they have been intensively studied as targets for potential anticancer therapeutics, producing a steady yearly rise in the number of published research articles. Many pyrazoline derivatives have shown remarkable cytotoxic activities in the form of heterocyclic or non-heterocyclic based hybrids, such as with coumarins, triazoles, and steroids. The enormous amount of related literature in the last 5 years prompted us to collect all these published data from screening against cancer cell lines, or protein targets like EGFR and structure activity relationship studies. Therefore, in the present review, a comprehensive account of the compounds containing the pyrazoline nucleus will be provided. The chemical groups and the structural modifications responsible for the activity will be highlighted. Moreover, emphasis will be given on recent examples from the literature and on the work of research groups that have played a key role in the development of this field.

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“…The in vitro anticancer activities of 2a – 2f and 3a – 3f were evaluated against two colon cancer cell lines to assess the influence of synthesised 1,3,5-triazine derivatives on cellular viability ( Table 1 ). Anticancer studies of 1,3,5-triazine derivatives is extensive, but only a few studies had performed their evaluations with HCT116 and SW620 cell lines [ 26 , 27 ]. Cisplatin was used as a positive control and the result was consistent with reported literature value [ 28 ].…”

Section: Resultsmentioning

confidence: 99%

Biguanide-Based Synthesis of 1,3,5-Triazine Derivatives with Anticancer Activity and 1,3,5-Triazine Incorporated Calcium Citrate Nanoparticles

et al. 2021

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Twelve derivatives of biguanide-derived 1,3,5-triazines, a promising class of anticancer agent, were synthesised and evaluated for their anticancer activity against two colorectal cancer cell lines—HCT116 and SW620. 2c and 3c which are the derivatives containing o-hydroxyphenyl substituents exhibited the highest activity with IC50 against both cell lines in the range of 20–27 µM, which is comparable to the IC50 of cisplatin reference. Moreover, the potential use of the calcium citrate nanoparticles (CaCit NPs) as a platform for drug delivery system was studied on a selected 1,3,5-triazine derivative 2a. Condition optimisation revealed that the source of citrate ions and reaction time significantly influence the morphology, size and %drug loading of the particles. With the optimised conditions, “CaCit-2a NPs” were successfully synthesised with the size of 148 ± 23 nm and %drug loading of up to 16.3%. Furthermore, it was found that the release of 2a from the synthesised CaCit-2a NPs is pH-responsive, and 2a could be control released under the acidic cancer environment. The knowledge from this study is perceptive for further development of the 1,3,5-triazine-based anticancer drugs and provide the platform for the incorporation of other drugs in the CaCit NPs in the future.

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Synthesis of New 1,3,5-Triazine-Based 2-Pyrazolines as Potential Anticancer Agents

Cited by 50 publications

References 39 publications

1,3,5‐Triazine: A versatile pharmacophore with diverse biological activities

1,3,5‐Triazine: A versatile pharmacophore with diverse biological activities

Pyrazoline Hybrids as Promising Anticancer Agents: An Up-to-Date Overview

Biguanide-Based Synthesis of 1,3,5-Triazine Derivatives with Anticancer Activity and 1,3,5-Triazine Incorporated Calcium Citrate Nanoparticles

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