scholarly journals Knigth's Move in the Periodic Table, From Copper to Platinum, Novel Antitumor Mixed Chelate Copper Compounds, Casiopeinas, Evaluated by an in Vitro Human and Murine Cancer Cell Line Panel

2001 ◽  
Vol 8 (1) ◽  
pp. 19-28 ◽  
Author(s):  
Isabel Gracia-Mora ◽  
Lena Ruiz-Ramírez ◽  
Celedonio Gómez-Ruiz ◽  
Mabel Tinoco-Méndez ◽  
Adriana Márquez-Quiñones ◽  
...  
Keyword(s):  
Cancer Cell ◽  
Anticancer Agents ◽  
Human Cancer ◽  
Cancer Cell Line ◽  
Drug Candidates ◽  
Control Drug ◽  
Copper Compounds ◽  
Structure Activity ◽  
Cell Line Panel

We synthesized a novel anticancer agents based on mixed chelate copper (II) complexes, named Casiopeínas® has of general formula [Cu(N-N)(N-O)H2O]NO3 (where, N-N = diimines as 1,10- phenanthroline, 2,2-bipyridine, or substituted and N-O=aminoeidate or [Cu(N-N)(O-O)H2O]NO3 (where NN= diimines as 10-phenanthroline, 2,2-bipyridine or substituted Casiopeínas I, II, IV, V, VI, VII VIII and O-O=acetylacetonate, salicylaldehidate Casiopínas III). We evaluated the in vitro antitumor activity using a human cancer cell panel and some nurine cancer cells. Eleven Casiopeinas are evaluated in order to acquire some structure-activity correlations and some monodentated Casiopeinäs analogues; cisplatinum was used as control drug. The 50% growth inhibition observed is, in all cases reach with concentrations of Casiopeina's 10 or 100 times lower than cisplatinum. In a previous work we reported the induction of apoptosis by Casiopeina II. The results indicate that Casiopeinass are a promising new anticancer drug candidates to be developed further toward clinical trials.

scholarly journals Synthesis and Experimental Validation of New Designed Heterocyclic Compounds with Antiproliferative Activity versus Breast Cancer Cell Lines MCF-7 and MDA-MB-231

2017 ◽  
Vol 2017 ◽  
pp. 1-10 ◽  
Author(s):  
Vincenza Barresi ◽  
Carmela Bonaccorso ◽  
Domenico A. Cristaldi ◽  
Maria N. Modica ◽  
Nicolò Musso ◽  
...  
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Cancer Cell Line ◽  
Breast Cancer Cell Lines ◽  
Design And Synthesis ◽  
Human Breast Cell ◽  
Mcf 7

Recent drug discovery efforts are highly focused towards identification, design, and synthesis of small molecules as anticancer agents. With this aim, we recently designed and synthesized novel compounds with high efficacy and specificity for the treatment of breast tumors. Based on the obtained results, we constructed a Volsurf+ (VS+) model using a dataset of 59 compounds able to predict the in vitro antitumor activity against MCF-7 cancer cell line for new derivatives. In the present paper, in order to further verify the robustness of this model, we report the results of the projection of more than 150 known molecules and 9 newly synthesized compounds. We predict their activity versus MCF-7 cell line and experimentally verify the in silico results for some promising chosen molecules in two human breast cell lines, MCF-7 and MDA-MB-231.

Novel N-bridged pyrazole-1-carbothioamides with potential antiproliferative activity: design, synthesis, in vitro and in silico studies

2021 ◽  
Vol 13 (20) ◽  
pp. 1743-1766
Author(s):  
Islam H El Azab ◽  
Essa M Saied ◽  
Alaa A Osman ◽  
Amir E Mehana ◽  
Hosam A Saad ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Antiproliferative Activity ◽  
In Silico ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Molecular Docking Study ◽  
In Silico Studies

Thiazole-substituted pyrazole is an important structural feature of many bioactive compounds, including antiviral, antitubercular, analgesic and anticancer agents. Herein we describe an efficient and facile approach for the synthesis of two series of 36 novel N-bridged pyrazole-1-phenylthiazoles. The antiproliferative activity of a set of representative compounds was evaluated in vitro against different human cancer cell lines. Among the identified compounds, compound 18 showed potent anticancer activity against the examined cancer cell lines. The in silico molecular docking study revealed that compound 18 possesses high binding affinity toward both SK1 and CDK2. Overall, these results indicate that compound 18 is a promising lead anticancer compound which may be exploited for development of antiproliferative drugs.

scholarly journals Suppressive Effect of Fig (Ficus Carica) Latex on Esophageal Cancer Cell Proliferation

2013 ◽  
Vol 30 (2) ◽  
pp. 93-96 ◽  
Author(s):  
Seyyed Abbas Hashemi ◽  
Saeid Abediankenari
Keyword(s):  
Esophageal Cancer ◽  
Cell Line ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Line ◽  
Ficus Carica ◽  
Esophageal Cancer Cell ◽  
Fig Tree ◽  
Vitro Effect

SUMMARY Fig (Ficus carica) tree latex was a source of treatment of different diseases in the Iranian traditional medicine reported by Avicenna in his 10th century book Canon of Medicine. The aim of this investigation was to establish the anticancer effect of fig tree latex on human cancer cells. The in vitro effect of different doses of fig tree latex including 2.5 mg/ml, 5 mg/ml, and 10 mg/ml on esophageal cancer cell line was evaluated after 72 hours by MTT assay. There was a significant change in 10 mg/ml treatment of latex after 72 hours on esophageal cancer line (P; 0.025). Ten mg/ml was the optimum concentration in the inhibition of cell line growth. Fig (Ficus carica) tree latex could be a candidate as a potential agent for the inhibition of cancerous cells production and development.

scholarly journals Synthesis, Spectral Characterization, and In Vitro Cytotoxicity of Some Fe(III) Complexes Bearing Unsymmetrical Salen-Type Ligands Derived from 2-Hydroxynaphthaldehyde and Substituted Salicylaldehydes

2021 ◽  
Vol 2021 ◽  
pp. 1-9
Author(s):  
Quang Trung Nguyen ◽  
Phuong Nam Pham Thi ◽  
Nguyen Van Tuyen
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Line ◽  
Tumor Cell Line ◽  
In Vitro Cytotoxicity ◽  
Ionization Mass ◽  
Hek 293 ◽  
Human Cancer Cell Lines

Six Fe(III) complexes bearing unsymmetrical salen-type ligands derived from 2-hydroxynaphthaldehyde and substituted salicylaldehydes were synthesized by coordinating the unsymmetrical salen-type ligands with FeCl3.6H2O. The synthetic complexes were characterized by electrospray ionization mass spectra (ESI-MS), effective magnetic moments (μeff), and infrared (IR) and ultraviolet-visible (UV-Vis) spectra. The spectroscopic data are in good agreement with the suggested molecular formulae of the complexes. Their cyclic voltammetric studies in acetonitrile solutions showed that the Fe(III)/Fe(II) reduction processes are electrochemically irreversible. The in vitro cytotoxicity of the obtained complexes was screened on human cancer cell lines KB (a subline of Hela tumor cell line) and HepG2 (a human liver cancer cell line) and a normal human cell line HEK-293 (Human Embryonic Kidney cell line). The results showed that the synthetic Fe(III) complexes are highly cytotoxic and quite selective. The synthetic complexes bearing unsymmetrical salen-type ligands with different substituted groups in the salicyl ring indicate different cytotoxicity.

Change in E-cadherin expression after X-ray irradiation of a human cancer cell line in vitro and in vivo

1998 ◽  
Vol 41 (3) ◽  
pp. 669-674 ◽  
Author(s):  
Takeshi Ebara ◽  
Norio Mitsuhashi ◽  
Yoshihiro Saito ◽  
Tetsuo Akimoto ◽  
Hideo Niibe
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Line ◽  
Human Cancer Cell Line ◽  
Human Cancer Cell ◽  
X Ray ◽  
E Cadherin

scholarly journals Potassium bicarbonate and D-ribose effects on A72 canine and HTB-126 human cancer cell line proliferation in vitro

2011 ◽  
Vol 11 (1) ◽  
pp. 30 ◽  
Author(s):  
Simonetta Croci ◽  
Luca Bruni ◽  
Simona Bussolati ◽  
Marianna Castaldo ◽  
Maurizio Dondi
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Line ◽  
Human Cancer Cell Line ◽  
Potassium Bicarbonate ◽  
Human Cancer Cell ◽  
Proliferation In Vitro

scholarly journals Evaluation of Synthetic 2,4-Disubstituted-benzo[g]quinoxaline Derivatives as Potential Anticancer Agents

2021 ◽  
Vol 14 (9) ◽  
pp. 853
Author(s):  
Islam Zaki ◽  
Sara A. Abu El-ata ◽  
Eman Fayad ◽  
Ola A. Abu Ali ◽  
Ali H. Abu Almaaty ◽  
...  
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Cancer Cell Line ◽  
Cell Cycle Profile ◽  
Quinoxaline Derivatives ◽  
New Compounds ◽  
Potent Inhibitory Activity ◽  
Mcf 7

A new series of 2,4-disubstituted benzo[g]quinoxaline molecules have been synthesized, using naphthalene-2,3-diamine and 1,4-dibromonaphthalene-2,3-diamine as the key starting materials. The structures of the new compounds were confirmed by spectral data along with elemental microanalyses. The cytotoxic activity of all synthesized benzo[g]quinoxaline derivatives was assessed in vitro against the breast MCF-7 cancer cell line. The tested molecules revealed good cytotoxicity toward the breast MCF-7 cancer cell line, especially compound 3. The results of topoisomerase IIβ inhibition assay revealed that compound 3 exhibits potent inhibitory activity in submicromolar concentration. Additionally, compound 3 was found to cause pre-G1 apoptosis, and slightly increase the cell population at G1 and S phases of the cell cycle profile in MCF-7 cells. Finally, compound 3 induces apoptosis via Bax activation and downregulation of Bcl2, as revealed by ELISA assay.

scholarly journals Anticolon Cancer Properties of Pyrazole Derivatives Acting through Xanthine Oxidase Inhibition

2021 ◽  
Vol 2021 ◽  
pp. 1-5
Author(s):  
Abdulrhman Alsayari ◽  
Yahya I. Asiri ◽  
Abdullatif Bin Muhsinah ◽  
Mohd. Zaheen Hassan
Keyword(s):  
Xanthine Oxidase ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Cancer Cell Line ◽  
Human Colon ◽  
Colon Cancer Cell Line ◽  
Pyrazole Derivatives ◽  
Anticancer Activities ◽  
Human Colon Cancer

Background. Pyrazoles are an interesting class of compounds showing potent anticancer activities. Our previous studies have demonstrated the potent anticancer activity of pyrazole analogues. Therefore, we focused on developing anticancer agents through structure optimization of the pyrazolyl lead molecule. Methods. The pyrazole derivatives were prepared by the appropriate synthetic protocols. The antiproliferative activities were evaluated using a sulforhodamine B assay against three cancer cell lines. In vitro and in silico molecular docking studies employing xanthine oxidase were used to explore the mechanism by which pyrazole derivatives exert anticancer effects. Results. One of the pyrazole derivatives demonstrated the greatest promise as an anticancer agent against the human colon cancer cell line (IC50 4.2 μM), with a potent xanthine oxidase inhibitory activity (IC50 0.83 μM). Conclusion. In summary, our findings suggest that these pyrazolyl analogues containing a pyridine nucleus could serve as a promising lead molecule in the development of novel anticancer agents.

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