scholarly journals Polyhydroxy Sterols Isolated from the Red Sea Soft Coral Lobophytum crassum and their Cytotoxic Activity

2017 ◽  
Vol 12 (2) ◽  
pp. 1934578X1701200
Author(s):  
Elsayed A. Aboutabl ◽  
Nabil M. Selim ◽  
Shadia M Azzam ◽  
Camilia G. Michel ◽  
Mohamed F. Hegazy ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Red Sea ◽  
Soft Coral ◽  
Human Cancer ◽  
Human Cancer Cell ◽  
Nmr Analysis ◽  
Human Cancer Cell Lines ◽  
Hct 116

One new (1) together with four known sterols (2 - 5) and a sesquiterpene (6) were isolated from a polar extract of the Red Sea soft coral Lobophytum crassum. The compounds were identified as 24-methylenecholest-5-ene-1α,3 1α,11α-triol 1-acetate (1), 24-methylenecholest-5-ene-1α,3β,11α-triol (2), 24-methylenecholest-5-ene-3β-ol (3), 24-methylenecholestane-1α,3β,5a,6P,1-pentol (4), 24-methylenecholestane-3β,5α,6β-triol (5) and alismoxide (6) based on extensive NMR analysis. The cytotoxicity of compounds 1 - 6 was evaluated in vitro using three human cancer cell lines viz., HepG2, Hep-2 and HCT-116. Compound 1 showed selective cytotoxic activity against HepG2, while 3 exhibited cytotoxicity against all tested cell lines.

scholarly journals Discovery of New Pyrazolopyridine, Furopyridine, and Pyridine Derivatives as CDK2 Inhibitors: Design, Synthesis, Docking Studies, and Anti-Proliferative Activity

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3923
Author(s):  
Adel A.-H. Abdel-Rahman ◽  
Amira K. F. Shaban ◽  
Ibrahim F. Nassar ◽  
Dina S. EL-Kady ◽  
Nasser S. M. Ismail ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Molecular Docking Study ◽  
Human Cancer Cell Lines ◽  
Hct 116 ◽  
Mcf 7

New pyridine, pyrazoloyridine, and furopyridine derivatives substituted with naphthyl and thienyl moieties were designed and synthesized starting from 6-(naphthalen-2-yl)-2-oxo-4-(thiophen-2-yl)-1,2-dihydropyridine-3-carbonitrile (1). The chloro, methoxy, cholroacetoxy, imidazolyl, azide, and arylamino derivatives were prepared to obtain the pyridine-−C2 functionalized derivatives. The derived pyrazolpyridine-N-glycosides were synthesized via heterocyclization of the C2-thioxopyridine derivative followed by glycosylation using glucose and galactose. The furopyridine derivative 14 and the tricyclic pyrido[3′,2′:4,5]furo[3,2-d]pyrimidine 15 were prepared via heterocyclization of the ester derivative followed by a reaction with formamide. The newly synthesized compounds were evaluated for their ability to in vitro inhibit the CDK2 enzyme. In addition, the cytotoxicity of the compounds was tested against four different human cancer cell lines (HCT-116, MCF-7, HepG2, and A549). The CDK2/cyclin A2 enzyme inhibitory results revealed that pyridone 1, 2-chloro-6-(naphthalen-2-yl)-4-(thiophen-2-yl)nicotinonitrile (4), 6-(naphthalen-2-yl)-4-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-amine (8), S-(3-cyano-6-(naphthaen-2-yl)-4-(thiophen-2-yl)pyridin-2-yl) 2-chloroethanethioate (11), and ethyl 3-amino-6-(naphthalen-2-yl)-4-(thiophen-2-yl)furo[2,3-b]pyridine-2-carboxylate (14) are among the most active inhibitors with IC50 values of 0.57, 0.24, 0.65, 0.50, and 0.93 µM, respectively, compared to roscovitine (IC50 0.394 μM). Most compounds showed significant inhibition on different human cancer cell lines (HCT-116, MCF-7, HepG2, and A549) with IC50 ranges of 31.3–49.0, 19.3–55.5, 22.7–44.8, and 36.8–70.7 μM, respectively compared to doxorubicin (IC50 40.0, 64.8, 24.7 and 58.1 µM, respectively). Furthermore, a molecular docking study suggests that most of the target compounds have a similar binding mode as a reference compound in the active site of the CDK2 enzyme. The structural requirements controlling the CDK2 inhibitory activity were determined through the generation of a statistically significant 2D-QSAR model.

scholarly journals Triangulene C, A New Cubitane-Based Diterpenoid from the Soft Coral Sinularia Triangula

2012 ◽  
Vol 7 (4) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Huey-Jen Su ◽  
Nai-Lun Lee ◽  
Mei-Chin Lu ◽  
Jui-Hsin Su
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Spectroscopic Data ◽  
Soft Coral ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Hct 116

A new cubitane-based diterpenoid, triangulene C (1), was isolated from the soft coral Sinularia triangula and its structure was elucidated on the basis of spectroscopic data. Compound 1 was not cytotoxic (IC50 >20 μg/mL) toward the four human cancer cell lines tested (HL60, MDA-MB-231, HCT-116 and DLD-1).

Screening of in vitro cytotoxic activity potential of Odontobuthus doriae and bothutus Saulcyi scorpion venoms against a panel of human cancer cell lines

Toxicon ◽  
2019 ◽  
Vol 158 ◽  
pp. S49
Author(s):  
Toktam M. Kashani ◽  
Amir Salarian ◽  
Hossein Vatanpour ◽  
Farshad Shirazi ◽  
Abbas Zare ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Scorpion Venoms

In vitro Cytotoxic Activity of Extracts and Isolated Constituents of Salvia leriifoliaBenth. against a Panel of Human Cancer Cell Lines

2011 ◽  
Vol 8 (6) ◽  
pp. 1152-1162 ◽  
Author(s):  
Rosa Tundis ◽  
Monica R. Loizzo ◽  
Federica Menichini ◽  
Marco Bonesi ◽  
Carmela Colica ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

Evaluation of the In Vitro Cytotoxic Activity of Jania rubens Against Jurkat and Molt-4 Human Cancer Cell Lines

2017 ◽  
Vol 1 (5) ◽  
pp. 199-202
Author(s):  
Rahamat Unissa ◽  
◽  
Sai Cheruvu ◽  
Mulakalapalli Tejaswi ◽  
Mareda Raghavi ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

Cytotoxic activity of ethanol extracts of in vitro grown Cistus creticus subsp. creticus L. on human cancer cell lines

2012 ◽  
Vol 38 ◽  
pp. 153-159 ◽  
Author(s):  
Marijana Skorić ◽  
Slađana Todorović ◽  
Nevenka Gligorijević ◽  
Radmila Janković ◽  
Suzana Živković ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Ethanol Extracts ◽  
Cistus Creticus

Copper(ii) complexes with benzhydrazone-related ligands: synthesis, structural studies and cytotoxicity assay

2017 ◽  
Vol 41 (6) ◽  
pp. 2425-2435 ◽  
Author(s):  
Marina Cindrić ◽  
Alen Bjelopetrović ◽  
Gordana Pavlović ◽  
Vladimir Damjanović ◽  
Jasna Lovrić ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Synthesis And Characterization ◽  
Structural Studies ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

The present study reports the synthesis and characterization of copper(ii) complexes with benzhydrazone-related ligands. They were screened for their cytotoxic activityin vitroin THP-1 and HepG2 human cancer cell lines.

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