ChemInform Abstract: Sesquiterpenes from Rhizomes of Cyperus rotundus with Cytotoxic Activities on Human Cancer Cells in vitro.

ChemInform ◽  
2016 ◽  
Vol 47 (8) ◽  
pp. no-no ◽  
Author(s):  
Byeol Ryu ◽  
Hye Mi Kim ◽  
Jae-Seung Lee ◽  
Yoon Jin Cho ◽  
Myung Sook Oh ◽  
...  
2021 ◽  
Vol 45 (11) ◽  
pp. 5176-5183
Author(s):  
Ichraf Slimani ◽  
Serap Şahin-Bölükbaşı ◽  
Mustafa Ulu ◽  
Enes Evren ◽  
Nevin Gürbüz ◽  
...  

A series of benzimidazolium salts and their [RhCl(NHC)(COD)] complexes were synthesized. All compounds were screened for in vitro cytotoxic activities against a panel of human cancer cells (HT-29 colon, Ishikawa endometrial, U-87 glioblastoma) using the MTT assay for 48 h incubation time.


Planta Medica ◽  
2015 ◽  
Vol 81 (16) ◽  
Author(s):  
B Ryu ◽  
HM Kim ◽  
JS Lee ◽  
YJ Cho ◽  
MS Oh ◽  
...  

Molecules ◽  
2019 ◽  
Vol 24 (9) ◽  
pp. 1780 ◽  
Author(s):  
Julio Benites ◽  
Jaime A. Valderrama ◽  
Maryan Ramos ◽  
Maudy Valenzuela ◽  
Angélica Guerrero-Castilla ◽  
...  

A broad range of 3-acyl-2,5-bis(phenylamino)-1,4-benzoquinones were synthesized and their voltammetric values, as well as in vitro cancer cell cytotoxicities, were assessed. The members of this series were prepared from acylbenzoquinones and phenylamines, in moderate to good yields (47–74%), through a procedure involving a sequence of two in situ regioselective oxidative amination reactions. The cyclic voltammograms of the aminoquinones exhibit two one-electron reduction waves to the corresponding radical-anion and dianion, and two quasi-reversible oxidation peaks. The first and second half-wave potential values (E1/2) of the members of the series were sensitive to the push-pull electronic effects of the substituents around the benzoquinone nucleus. The in vitro cytotoxic activities of the 3-acyl-2,5-bis(phenylamino)-1,4-benzoquinones against human cancer cells (bladder and prostate) and non-tumor human embryonic kidney cells were measured using the MTT colorimetric method. The substitution of both aniline groups, by either methoxy (electron donating effect) or fluorine (electron withdrawal effect), decreased the cytotoxicity in the aminoquinones. Among the members of the unsubstituted phenylamino series, two of the 18 compounds showed interesting anti-cancer activities. A preliminary assay, looking for changes in the expression of selected genes, was performed. In this context, the two compounds increased TNF gene expression, suggesting an association with an inflammatory-like response.


2020 ◽  
Vol 2020 ◽  
pp. 1-11
Author(s):  
David Ríos ◽  
Jaime A. Valderrama ◽  
Miriam Cautin ◽  
Milko Tapia ◽  
Felipe Salas ◽  
...  

The reaction of 2-acyl-1,4-naphthoquinones with N,N-dimethylaniline and 2,5-dimethoxyaniline, promoted by catalytic amounts of CeCl3·7H2O under “open-flask” conditions, produced a variety of 2-acyl-3-aminophenyl-1,4-naphthoquinones structurally related to the cytotoxic 2-acetyl-3-phenyl-1,4-naphthoquinone, an inhibitor of the heat shock chaperone protein Hsp90. The members of the 2-acyl-3-aminophenyl-1,4-naphthoquinone series were isolated in good yields (63-98%). The cyclic voltammograms of the 2-acyl-3-aminophenyl-1,4-naphthoquinone exhibit two one-electron reduction waves to the corresponding radical-anion and dianion and two quasireversible oxidation peaks. The first and second half-wave potential values (E1/2) of the members of the series are sensitive to the push-pull electronic effects of the substituents in the naphthoquinone scaffold. Furthermore, the in vitro antiproliferative properties of these new quinones were evaluated on two human cancer cells DU-145 (prostate) and MCF-7 (mammary) and a nontumorigenic HEK-293 (kidney) cell line, using the MTT colorimetric method. Two members, within the series, exhibited interesting cytotoxic activities on human prostate and mammary cancer cells.


2021 ◽  
Vol 22 (16) ◽  
pp. 8372
Author(s):  
Ana María Zárate ◽  
Christian Espinosa-Bustos ◽  
Simón Guerrero ◽  
Angélica Fierro ◽  
Felipe Oyarzún-Ampuero ◽  
...  

The Smoothened (SMO) receptor is the most druggable target in the Hedgehog (HH) pathway for anticancer compounds. However, SMO antagonists such as vismodegib rapidly develop drug resistance. In this study, new SMO antagonists having the versatile purine ring as a scaffold were designed, synthesised, and biologically tested to provide an insight to their mechanism of action. Compound 4s was the most active and the best inhibitor of cell growth and selectively cytotoxic to cancer cells. 4s induced cell cycle arrest, apoptosis, a reduction in colony formation and downregulation of PTCH and GLI1 expression. BODIPY-cyclopamine displacement assays confirmed 4s is a SMO antagonist. In vivo, 4s strongly inhibited tumour relapse and metastasis of melanoma cells in mice. In vitro, 4s was more efficient than vismodegib to induce apoptosis in human cancer cells and that might be attributed to its dual ability to function as a SMO antagonist and apoptosis inducer.


2021 ◽  
Vol 16 (2) ◽  
pp. 1934578X2199615
Author(s):  
Lucas Botelho Jerônimo ◽  
Jamile S. da Costa ◽  
Laine C. Pinto ◽  
Raquel C. Montenegro ◽  
William N. Setzer ◽  
...  

This work analyzed the chemical compositions and evaluated the antioxidant and cytotoxic activities of essential oils (EO) of Eugenia patrisii (Epat), Eugenia stipitata (Esti), Myrcia splendens (Mspl), Myrcia sylvatica (Msyl), Psidium guajava (Pgua), and Psidium guineense (Pgui-1 and Pgui-2) from the Brazilian Amazon. Sesquiterpenoids were found in high concentrations in the oils of E. patrisii and M. splendens, which were rich in E-caryophyllene (32.0% and 45.8%); E. stipitata and M. sylvatica, which displayed germacrene D (11.8%) and germacrene B (24.5%); and P. guajava that showed epi-β-bisabolol (16.1%) as the main compound. However, P. guineense samples (Pgui-1 and Pgui-2) were rich in monoterpenoids such as limonene (Pgui-1: 30.2%; Pgui-2 30.4%) and α-pinene (Pgui-1: 22.5%; Pgui-2: 17.7%). The samples showed a weak and moderate antioxidant activities in the DPPH assay, displaying inhibition rates from 11.5% to 38.6% (at 10 mg/mL). All samples were cytotoxic against human cancer cells by the MTT method. Epat oil showed higher activity against melanoma (SKMEL-19, IC505.8 µg/mL), gastric (AGP01, IC503.2 µg/mL), and colon (HCT116, IC506.7 µg/mL). Meanwhile, the samples Pgua and Pgui were more active against breast cancer cells (MCF7, IC5012.4 µg/mL and 11.6 µg/mL, respectively).


2015 ◽  
Vol 3 (3) ◽  
pp. 457-468 ◽  
Author(s):  
Ishita Matai ◽  
Abhay Sachdev ◽  
P. Gopinath

Herein, we report the development of a poly(amidoamine) (PAMAM) dendrimer based multicomponent therapeutic agent forin vitrocancer therapy applications.


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