Hydroxyethylamide substituted triterpenoic acids hold good cytotoxicity for human tumor cells

Denner, Toni C.; Hoenke, Sophie; Kraft, Oliver; Deigner, Hans‐Peter; Al‐Harrasi, Ahmed; Csük, René

doi:10.1016/j.rechem.2022.100371

Cited by 6 publications

(1 citation statement)

References 56 publications

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“…Since previous work also indicated an effect on mitochondrial permeability transition [ 35 ], it was natural to transfer our own previous findings on pentacyclic triterpenes to the diterpene isosteviol. Of particular interest were benzyl and pyridine-amides, (iso)-quinoline amides, and especially (homo)-piperazinyl-spacered rhodamine B and rhodamine 101 conjugates [ 39 , 40 , 41 , 42 , 43 , 44 , 45 , 46 , 47 , 48 , 49 , 50 , 51 , 52 , 53 , 54 , 55 , 56 , 57 , 58 ].…”

Section: Introductionmentioning

confidence: 99%

The Finally Rewarding Search for A Cytotoxic Isosteviol Derivative

et al. 2023

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Acid hydrolysis of stevioside resulted in a 63% yield of isosteviol (1), which served as a starting material for the preparation of numerous amides. These compounds were tested for cytotoxic activity, employing a panel of human tumor cell lines, and almost all amides were found to be non-cytotoxic. Only the combination of isosteviol, a (homo)-piperazinyl spacer and rhodamine B or rhodamine 101 unit proved to be particularly suitable. These spacered rhodamine conjugates exhibited cytotoxic activity in the sub-micromolar concentration range. In this regard, the homopiperazinyl-spacered derivatives were found to be better than those compounds with piperazinyl spacers, and rhodamine 101 conjugates were more cytotoxic than rhodamine B hybrids.

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Section: Introductionmentioning

confidence: 99%

The Finally Rewarding Search for A Cytotoxic Isosteviol Derivative

et al. 2023

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An overview of the latest outlook of sulfamate derivatives as anticancer candidates (2020–2024)

Mustafa,

Shahin,

Alrashed

et al. 2024

Archiv der Pharmazie

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Considering the emergence of new anticancer drugs, in this review we emphasized and highlighted the recent reports and advances related to sulfamate‐incorporating compounds with potential anticancer activity during the last 5 years (2020–2024). Additionally, we discussed their structure–activity relationship, clarifying their potent bioactivity as anticancer agents. Sulfamate derivatives hold promise as effective therapeutic candidates against cancer. By targeting biological targets associated with the development of cancer, such as steroid sulfatases (STS), carbonic anhydrases (CAs), microtubules, NEDD8‐activating enzyme, small ubiquitin‐like modifiers (SUMO)‐activating enzyme (SAE), cyclin‐dependent kinases (CDKs), breast cancer susceptibility gene 1 (BRCA1), and so on, this can furnish small molecules as anticancer lead candidates serving the drug discovery field. For example, compound 2, an STS inhibitor, demonstrated superior activity compared to its reference, irosustat, by fivefold. In addition, compound 21, an SAE, is under phase I clinical trials. Continued research into sulfamate derivatives holds potential for the development of novel therapeutic agents targeting various diseases.

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