An insight into the therapeutic potential of piperazine-based anticancer agents

Walayat, Kamran; Mohsin, Noor ul Amin; Aslam, Sana; Ahmad, Matloob

doi:10.3906/kim-1806-7

Cited by 29 publications

(16 citation statements)

References 64 publications

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“…Moreover, organic and inorganic precursors holding sulfone entity were found to have promising potential as biological active agents, whereas piperazine analgoues have been proposed to be a key factor enhancing biological effects of the bearing molecules. Most important, the piperazine‐based anticancer agents include abemaciclib, bosutinib, brigatinib, dexrazoxane, dosatinib, imatinib, leucovorin, olaparib, palbociclib, ponatinib, rociletinib, venetoclax, and trabectidin, and so forth . Thus, we have aimed to prepare chrysin‐sulfonylpiperazine derivatives in the present research to gain enhanced biological significance.…”

Section: Introductionmentioning

confidence: 87%

Sulfonylpiperazines based on a flavone as antioxidant and cytotoxic agents

Patel

Mistry

Syed

et al. 2019

Archiv der Pharmazie

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Chrysin-based sulfonylpiperazines 7a-k were synthesized and investigated for their in vitro free radical scavenging potential as well as cytotoxic efficacies against selected cancer cell lines. Cytotoxicity of the new compounds toward noncancer cells was confirmed using the SRB assay against Madin-Darby Canine Kidney cells.Reaction of piperazine with different substituted benzenesulfonyl chlorides in triethylamine furnished sulfonylpiperazines (3a-k), which were then allowed to react with 7-(4-bromobutoxy)-5-hydroxy-2-phenyl-4H-chromen-4-one (6) prepared reacting chrysin with 1,4-dibromobutane to give the final derivatives 7a-k. The results concluded that chrysin-sulfonylpiperazines exerted better antioxidant and anticancer efficacies than previously studied chrysin-piperazine precursors. For example, compounds 7h, 7j, and 7k with 4-OCF 3 , 4-OCH 3 , and 2,4-diOCH 3 groups exhibited the best antioxidant potential against 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radicals. Moreover, halogenated analogues (7b, 7c, 7g, and 7h) demonstrated promising anticancer potential against SK-OV3, HeLa, and HT-29 cell lines, whereas those bearing a methoxy functional group (7j and 7k) had beneficial effects against the cell lines A-549 and HT-29. Thus, it can be confirmed from the bioassay results that the overall structural design as well as proper substitution is crucial to deliver the anticipated biological effects. Spectroscopic techniques such as FT-IR, 1 H NMR, 13 C NMR, mass and elemental analysis (CHN) were carried out to confirm the final structures.

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Section: Introductionmentioning

confidence: 87%

Sulfonylpiperazines based on a flavone as antioxidant and cytotoxic agents

Patel

Mistry

Syed

et al. 2019

Archiv der Pharmazie

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“…The piperazine is a nitrogen-containing heterocyclic ring known for its medicinal importance. It is considered the most attractive scaffold for the development of novel anticancer agents [97]. In 2016, Rathi and co-workers [98] 61) were synthesized by Zhao et al [99].…”

Section: Piperazinementioning

confidence: 99%

Pentacyclic Triterpenoids with Nitrogen-Containing Heterocyclic Moiety, Privileged Hybrids in Anticancer Drug Discovery

et al. 2021

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Pentacyclic triterpenoids are well-known phytochemicals with various biological activities commonly found in plants as secondary metabolites. The wide range of biological activities exhibited by triterpenoids has made them the most valuable sources of pharmacological agents. A number of novel triterpenoid derivatives with many skeletal modifications have been developed. The most important modifications are the formation of analogues or derivatives with nitrogen-containing heterocyclic scaffolds. The derivatives with nitrogen-containing heterocyclic compounds are among the most promising candidate for the development of novel therapeutic drugs. About 75% of FDA-approved drugs are nitrogen-containing heterocyclic moieties. The unique properties of heterocyclic compounds have encouraged many researchers to develop new triterpenoid analogous with pharmacological activities. In this review, we discuss recent advances of nitrogen-containing heterocyclic triterpenoids as potential therapeutic agents. This comprehensive review will assist medicinal chemists to understand new strategies that can result in the development of compounds with potential therapeutic efficacy.

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“…Therefore, piperazine derivatives are reported to possess a wide range of pharmacological properties [51,52] the most predominant being the anti-helminthic [53]. Other activities like anti-allergic [54], antimalarial [55][56][57], antimicrobial [58][59][60], antiemetic [61], antipsychotic [62], anticancer [63][64][65], anti-Alzheimer's [66,67], antihelminthic [68,69], CNS activities [70] etc. are also reported.…”

Section: Compound 2 R Ear Edema % Inhibitionmentioning

confidence: 99%

Piperazine: A Promising Scaffold with Analgesic and Anti-inflammatory Potential

et al. 2020

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Piperazine, a nitrogen-containing heterocyclic has acquired an inimitable position in medicinal chemistry because of its versatile structure, which has fascinated researchers to design novel piperazine based molecules having various biological actions. The subsistence of various compounds possessing diverse pharmacological activities in the literature further confirms this fact. Currently available analgesics and anti-inflammatory drugs are associated with side effects that limit their use. Moreover, the literature reveals the incredible anti-inflammatory and analgesic potential of piperazine derivatives along with their method of synthesis, therefore; the present review has been designed to collate the development made in this area that will surely be advantageous in designing novel piperazine based candidates with enhanced efficacy and less toxicity. An extensive literature survey was carried by scrutinizing peer reviewed articles from worldwide scientific databases available on GOOGLE, SCOPUS, PUBMED, and only relevant studies published in English were considered.

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An insight into the therapeutic potential of piperazine-based anticancer agents

Cited by 29 publications

References 64 publications

Sulfonylpiperazines based on a flavone as antioxidant and cytotoxic agents

Sulfonylpiperazines based on a flavone as antioxidant and cytotoxic agents

Pentacyclic Triterpenoids with Nitrogen-Containing Heterocyclic Moiety, Privileged Hybrids in Anticancer Drug Discovery

Piperazine: A Promising Scaffold with Analgesic and Anti-inflammatory Potential

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