One-pot synthesis and antiproliferative activity of novel 2,4-diaminopyrimidine derivatives bearing piperidine and piperazine moieties

Ma, Wenxue; Yang, Hai‐Kui; Hu, Meng-Jin; Li, Qian; Ma, Tianzhu; Zhou, Zhong‐Zhen; Liu, Ruiyuan; Wang, You; Zhao, Pei‐Liang

doi:10.1016/j.ejmech.2014.07.017

Cited by 25 publications

(7 citation statements)

References 31 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…In our study, in accordance, with these studies a high IC50 of 0.4 ± 0.03 mg/mL was found for 5-FU on the HCT116 colon cancer cell line. Ma et al found an IC50 value of 46.83 μM for 5-FU on HEPG2 cells [24] whereas our finding was 0.47 ± 0.02 mg/mL on the same cells.…”

Section: Expression Of Proteins Related To Apoptotic Pathways In Avg contrasting

confidence: 92%

Evaluation of Aloe Vera Leaf Extracts and Aloe Emodin on Several Cancer Cell Lines

Akev¹

2020

FARMACIA

View full text Add to dashboard Cite

Fresh leaf skin aqueous and methanolic extracts as well as shade-dried leaf skin methanolic extracts prepared separately from the leaves of Aloe vera and aloe emodin (AE) were assayed on human gastric (AGS), colon (HT-29, HCT116) and hepatocellular (HEPG2) cancer cell lines relative to human umbilical vein endothelial cells (HUVEC). AE, 5-fluorouracil (5-FU) and imatinib (IM) were tested as positive controls. Among the four extracts studied, A. vera gel extract (AVG) had the highest cytotoxic effect on cancer cells, with the highest effect on HCT116 cells, while no cytotoxic effect on HUVEC cells was detected. AE has also selective cytotoxic and apoptotic effects on the cancer cells and was ineffective on normal cells. AVG treatment in HCT116 cells induced the apoptosis by the activation of caspase-9 and caspase-3. According to our results, AVG and AE could be proposed as promising cytotoxic drugs from natural origin. Rezumat Extractele apoase și metanolice ale frunzelor proaspete, precum și extractele metanolice ale frunzelor uscate de Aloe vera și aloe emodin (AE) au fost analizate pe linii celulare canceroase gastrice (AGS), de colon (HT-29, HCT116) și hepatocelulare (HEPG2) față de celulele endoteliale ale venei ombilicale umane (HUVEC). AE, 5-fluorouracil (5-FU) și imatinib (IM) au fost martori pozitivi. Dintre cele patru extracte studiate, extractul de A. vera gel (AVG) a prezentat efect citotoxic superior asupra celulelor canceroase, în special asupra celulelor HCT116, și nici un efect citotoxic asupra celulelor HUVEC. AE are, de asemenea, efecte selective citotoxice și apoptotice asupra celulelor canceroase. Tratamentul cu AVG asupra celulelelor HCT116 a indus apoptoza prin activarea caspazei-9 și a caspazei-3. În concluzie, AVG și AE prezintă potențial chimioterapic promițător pentru terapia cancerului.

show abstract

Section: Expression Of Proteins Related To Apoptotic Pathways In Avg contrasting

confidence: 92%

Evaluation of Aloe Vera Leaf Extracts and Aloe Emodin on Several Cancer Cell Lines

Akev¹

2020

FARMACIA

View full text Add to dashboard Cite

show abstract

“…This work aims to obtain two new Cu(I)–I coordination polymers with Cu 2 I 2 double chains and 2,4-diaminopyridine . Their optical and electrical properties have been studied.…”

Section: Introductionmentioning

confidence: 99%

“…22 This work aims to obtain two new Cu(I)−I coordination polymers with Cu 2 I 2 double chains and 2,4-diaminopyridine. 34 Their optical and electrical properties have been studied. Additionally, their behavior versus external stimuli (pressure and temperature) has been measured and explained according to theoretical calculations.…”

Section: ■ Introductionmentioning

confidence: 99%

Cu(I)–I-2,4-diaminopyrimidine Coordination Polymers with Optoelectronic Properties as a Proof of Concept for Solar Cells

et al. 2020

View full text Add to dashboard Cite

Two coordination polymers with formulas [CuI(dapym)] n and [Cu 2 I 2 (dapym)] n (dapym = 2,4-diaminopyrimidine) have been synthesized in water at room temperature. According to the stoichiometry used, mono (1D) and the two-dimensional (2D) structures can be obtained. Both are made up of Cu 2 I 2 double chains. Their high insolubility in the reaction medium also makes it possible to obtain them on a nanometric scale. Their structural flexibility and short Cu−Cu distances provoke interesting optoelectronic properties and respond to physical stimuli such as pressure and temperature, making them interesting for sensor applications. The experimental and theoretical studies allow us to propose different emission mechanisms with different behaviors despite containing the same organic ligand. These behaviors are attributed to their structural differences. The emission spectra versus pressure and temperature suggest competencies between different transitions, founding critical Cu 2 I 2 environments, i.e., symmetric in the 1D compound and asymmetric for the 2D one. The intensity in the 2D compound's emission increases with decreasing temperature, and this behavior can be rationalized with a structural constriction that decreases the Cu−Cu and Cu−I distances. However, compound 1D exhibits a contrary behavior that may be related to a change of the organic ligand's molecular configuration. These changes imply that a more significant Π−Π interaction counteracts the contraction in distances and angles when the temperature decreased. Also, the experimental conductivity measurements and theoretical calculations show a semiconductor behavior. The absorption of the 1D compound in UV, its intense emission at room temperature, and the reduction to nanometric size have allowed us to combine it homogeneously with ethyl vinyl acetate (EVA), creating a new composite material. The external quantum efficiency of this material in a Si photovoltaic mini-module has shown that this compound is an active species with application in solar cells since it can move the photons of the incident radiation (UV region) to longer wavelengths.

show abstract

“…It is well known that pyrimidine core has wide occurrence in nature4, and which has also represent a typical class of heterocyclic scaffold in various compounds applied in the field of medicinal chemistry56789101112131415, agrochemicals161718192021222324, and materials2526272829. Up to now, many pyrimidines analogues have been demonstrated to exhibit wide pharmacological activities mainly including anticancer, antiviral, antibacterial, antimalarial, antituberculosis activities.…”

mentioning

confidence: 99%

Steroidal[17,16-d]pyrimidines derived from dehydroepiandrosterone: A convenient synthesis, antiproliferation activity, structure-activity relationships, and role of heterocyclic moiety

Shi

Zhang

et al. 2017

Sci Rep

View full text Add to dashboard Cite

A series of steroidal[17,16-d]pyrimidines derived from dehydroepiandrosterone were designed and prepared by a convenient heterocyclization reaction. The in vitro anticancer activities for these obtained compounds were evaluated against human cancer cell lines (HepG2, Huh-7, and SGC-7901), which demonstrated that some of these heterocyclic pyrimidine derivatives exhibited significantly good cytotoxic activities against all tested cell lines compared with 5-fluorouracil (5-FU), especially, compound 3b exhibited high potential growth inhibitory activities against all tested cell lines with the IC50 values of 5.41 ± 1.34, 5.65 ± 1.02 and 10.64 ± 1.49 μM, respectively, which might be used as promising lead scaffold for discovery of novel anticancer agents.

show abstract

One-pot synthesis and antiproliferative activity of novel 2,4-diaminopyrimidine derivatives bearing piperidine and piperazine moieties

Cited by 25 publications

References 31 publications

Evaluation of Aloe Vera Leaf Extracts and Aloe Emodin on Several Cancer Cell Lines

Evaluation of Aloe Vera Leaf Extracts and Aloe Emodin on Several Cancer Cell Lines

Cu(I)–I-2,4-diaminopyrimidine Coordination Polymers with Optoelectronic Properties as a Proof of Concept for Solar Cells

Steroidal[17,16-d]pyrimidines derived from dehydroepiandrosterone: A convenient synthesis, antiproliferation activity, structure-activity relationships, and role of heterocyclic moiety

Contact Info

Product

Resources

About