scholarly journals Biological Activity and In Silico Study of 3-Modified Derivatives of Betulin and Betulinic Aldehyde

2019 ◽  
Vol 20 (6) ◽  
pp. 1372 ◽  
Author(s):  
Ewa Bębenek ◽  
Elwira Chrobak ◽  
Krzysztof Marciniec ◽  
Monika Kadela-Tomanek ◽  
Justyna Trynda ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Human Cancer ◽  
Pharmacokinetic Profile ◽  
Breast Adenocarcinoma ◽  
Human Cancer Cell Lines ◽  
In Silico Study ◽  
Docking Calculations ◽  
Protein Kinase Akt ◽  
Derivatives Of ◽  
Mcf 7

A series of 3-substituted derivatives of betulin and betulinic aldehyde were synthesized as promising anticancer agents. The newly triterpenes were tested against five human cancer cell lines like biphenotypic B myelomonocytic leukaemia (MV-4-11), adenocarcinoma (A549), prostate (Du-145), melanoma (Hs294T), breast adenocarcinoma (MCF-7) and normal human mammary gland (MCF-10A). The compound 9 showed towards Du-145, MCF-7 and Hs294T cells significant antiproliferative activity with IC50 ranging from 7.3 to 10.6 μM. The evaluation of ADME properties of all compounds also includes their pharmacokinetic profile. The calculated TPSA values for synthetized derivatives are in the range between 43.38 Å2 and 55.77 Å2 suggesting high oral bioavailability. The molecular docking calculations showed that triterpene 9 fits the active site of the serine/threonine protein kinase Akt.

scholarly journals Synthesis and Anticancer Evaluations of Novel Thiazole Derivatives Derived from 4-Phenylthiazol-2-amine

2021 ◽  
Vol 68 (3) ◽  
pp. 604-616
Author(s):  
Amira E. M. Abdallah ◽  
Rafat M. Mohareb ◽  
Maher H. E. Helal ◽  
Germeen J. Mofeed
Keyword(s):  
Anticancer Agents ◽  
Human Cancer ◽  
Human Cell Line ◽  
Breast Adenocarcinoma ◽  
Small Cell Lung ◽  
Thiazole Derivatives ◽  
Human Cancer Cell Lines ◽  
Chemical Reagents ◽  
Cns Cancer ◽  
Mcf 7

Many novel thiazole derivatives were designed and synthesized using 4-phenylthiazol-2-amine. The reactivity of the latter compound toward different chemical reagents was studied. The structure of the newly synthesized compounds was established based on elemental analysis and spectral data. Furthermore, twenty compounds of the synthesized systems were selected and evaluated in (μM) as significant anticancer agents towards three human cancer cell lines [MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer), and SF-268 (CNS cancer)] and normal fibroblasts human cell line (WI-38). The results showed that compounds 9 and 14a displayed higher effeciency than the reference doxorubicin.

Synthesis and antiproliferative and c-Src kinase inhibitory activities of cinnamoyl- and pyranochromen-2-one derivatives

2013 ◽  
Vol 91 (8) ◽  
pp. 741-754 ◽  
Author(s):  
Karam Chand ◽  
Amir Nasrolahi Shirazi ◽  
Preeti Yadav ◽  
Rakesh K. Tiwari ◽  
Meena Kumari ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Kinase Inhibitors ◽  
Human Cancer ◽  
Src Kinase ◽  
Cancer Cell Lines ◽  
Ovarian Adenocarcinoma ◽  
Human Cancer Cell Lines ◽  
Mcf 7

A series of 6- and 8-cinnamoylchromen-2-one and dihydropyranochromen-2-one derivatives were synthesized and their antiproliferative activities were evaluated against three human cancer cell lines, i.e., ovarian adenocarcinoma (SK-OV-3), leukemia (CCRF-CEM), and breast carcinoma (MCF-7). In general, 8-cinnamoylchromen-2-one derivatives were found to have higher antiproliferative activity against the cancer cells when compared with 6-cinnamoyl analogues. Among all of the hybrid chromen-2-one − chalcone/flavanone compounds, a 7-hydroxy-8-cinnamoylchromen-2-one derivative 35 was found to be consistently active against all the cancer cell lines and inhibited the cell proliferation of SK-OV-3, CCRF-CEM, and MCF-7 by 63%, 50%, and 43%, respectively, at a concentration of 50 μmol/L after 72 h of incubation. This compound also exhibited the highest Src kinase inhibition (IC50 = 14.5 μmol/L). Structure−activity relationship studies provided insights for designing the next generation of chromen-2-one − chalcone hybrid prototypes and the development of new leads as anticancer agents and (or) Src kinase inhibitors.

CYTOTOXIC ACTIVITY OF LUVUNGA SCANDENS AGAINST HUMAN CANCER CELL LINES

2016 ◽  
Vol 78 (10) ◽  
Author(s):  
Putri Nur Hidayah Al-Zikri ◽  
Muhammad Taher ◽  
Deny Susanti ◽  
Solachuddin Jauhari Arief Ichwan
Keyword(s):  
Cytotoxic Activity ◽  
Cell Line ◽  
Cell Lines ◽  
A549 Cell ◽  
Human Cancer ◽  
In Vitro Cytotoxicity ◽  
Breast Adenocarcinoma ◽  
Human Cancer Cell Lines ◽  
Mcf 7

Luvunga scandens belongs to the family of Rutaceae which usually inhabit tropical and moist environment. This plant is known as ‘Mengkurat Jakun’ among locals and used traditionally to treat fever and fatigue via decoction. The aim of this study was to investigate the cytotoxic activity of the leaves and stems extracts of L. scandens extract. Extracts of the leaves and stems were obtained from sequential extraction procedures by various organic solvents. All extracts were subjected to cytotoxic study by 3-(4, 5-dimethylthaizol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. In in vitro cytotoxicity assay, all L. scandens extracts exhibited cytotoxicity against human breast adenocarcinoma (MCF-7) and human lung adenocarcinoma (A549) cell lines. The IC50 values of dichloromethane and methanol extracts from the leaves of L. scandens against MCF-7 cell line were 62.5 µg/mL and 88.0 µg/mL, respectively, whereas IC50 of methanol extract from stem was 81.0 µg/mL. All extracts were less active against A549 cell line where IC50 value were not be determined. The present findings revealed the potential of L. scandens as a cytotoxic agent against MCF-7 cell line. However, further studies should be planned to evaluate role of the plant in cytotoxic activity.

scholarly journals Design, Synthesis, and Cytotoxic Evaluation of Novel Lupane Triterpenoid Derived Hydroxamates

2020 ◽  
Vol 15 (6) ◽  
pp. 1934578X2093196
Author(s):  
Dang Thi Tuyet Anh ◽  
Dinh Thi Cuc ◽  
Le Nhat Thuy Giang ◽  
Nguyen Thi Hien ◽  
Vu Ngoc Doan ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Human Cancer ◽  
Human Cancer Cell ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Lupane Triterpenoids ◽  
Lead Compounds ◽  
Diphenyltetrazolium Bromide ◽  
Derivatives Of

A series of new hydroxamate derivatives of lupane triterpenoids has been designed and successfully synthesized. The synthesized compounds were evaluated for their in vitro antitumor activity using the 3-[4,5-dimethylthiazol-2-yl]−2,5-diphenyltetrazolium bromide-based assay against the human cancer cell lines KB and HepG2. Most of these derivatives possess at least moderate cytotoxic activity and the hydroxamate derivative compounds 3c, 3e, 7a, and 15b could be lead compounds for further optimization to develop novel anticancer agents.

scholarly journals Synthesis, cytotoxicity, and molecular docking of methylated (–)-epigallocatechin-3-gallate-4β-triazolopodophyllotoxin derivatives as novel antitumor agents

2021 ◽  
pp. 174751982110273
Author(s):  
Cheng-Ting Zi ◽  
Ze-Hao Wang ◽  
Jing Shi ◽  
Bo-Ya Shi ◽  
Ning Zhang ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Anticancer Agents ◽  
Antitumor Agents ◽  
Click Reaction ◽  
Human Cancer ◽  
Growth Factor Receptor ◽  
Human Cancer Cell Lines ◽  
Epidermal Growth ◽  
Further Development ◽  
Mcf 7

A series of novel methylated (–)-epigallocatechin-3-gallate-4β-triazolopodophyllotoxin derivatives is synthesized by utilizing the click reaction. Evaluation of their cytotoxicity against a panel of five human cancer cell lines (HL-60, SMMC-7721, A-549, MCF-7, and SW480) using the MTT assay shows that most of these compounds exhibit weak cytotoxicity. It is observed that compound 12 shows the highest activity against A-549 cells with an IC50 value of 10.27 ± 0.90 μM. Molecular docking results suggested that this compound 12 has a higher binding affinity for epidermal growth factor receptor than for tubulin. Our findings support the utility of compound 12 as a novel compound for the further development of anticancer agents.

Novel 1,3,4-Thiadiazole Linked Amide Derivatives of Pteridone: Synthesis and Study of Anticancer Activities

2019 ◽  
Vol 17 (1) ◽  
pp. 54-60
Author(s):  
Eeduri R. Devi ◽  
Reddymasu Sreenivasulu ◽  
Koya P. Rao ◽  
Ratnakaram V. Nadh ◽  
Malladi Sireesha
Keyword(s):  
Cell Lines ◽  
Human Cancer ◽  
Positive Control ◽  
Anticancer Activities ◽  
Human Cancer Cell Lines ◽  
Mtt Method ◽  
Amide Derivatives ◽  
Derivatives Of ◽  
A549 Lung ◽  
Mcf 7

Cancer is a second leading cause of death after heart attack, in developing as well as undeveloped countries. It is caused by unregulated growth and metastasis of the abnormal cancer cells. Cancer can be cured by radiation, immunotherapy and chemotherapy, among them; chemotherapy is a good treatment for cancer, in which chemotherapeutic drug is used. The anticancer activity of newly synthesized compounds (13a-j) was carried out on four different types of human cancer cell lines like MCF-7 (breast), A549 (lung), Colo-205 (colon) and A2780 (ovarian) by the MTT method, and compared to etoposide used as a positive control. Among them, compound 13g with electron-withdrawing (3,5-dinitro) group, exhibited more promising activity in all cell lines (MCF-7 = 0.10±0.076 µM, A549 = 0.17±0.039 µM, Colo-205= 0.13±0.022 µM and A2780 = 0.87±0.027µM). This compound may act as lead drug in cancer chemotherapy. In future, this compound can be examined for clinical studies.

Nitroimidazoles Part 9. Synthesis, molecular docking, and anticancer evaluations of piperazine-tagged imidazole derivatives

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Yaseen A. Al-Soud ◽  
Ala’a H. Al-Ahmad ◽  
Luay Abu-Qatouseh ◽  
Amneh Shtaiwi ◽  
Kafa’ A. S. Alhelal ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Anticancer Agents ◽  
Human Cancer ◽  
Dermal Fibroblast ◽  
Hepg2 Cell Line ◽  
Alkyl Aryl ◽  
Human Cancer Cell Lines ◽  
Imidazole Derivatives ◽  
Inhibition Potency ◽  
Mcf 7

Abstract New piperazine-tagged imidazole derivatives were synthesized via reaction of 1-alkyl/aryl-5-bromo-2-alkyl-4-nitro-1H-imidazoles 1–3 with piperazine nucleophiles. Nine selected compounds were assessed for their antiproliferative inhibition potency against five human cancer cell lines (MCF-7, PC3, Du145, HepG2 and Dermal/Fibroblast). Compounds 7 and 10 are the most potent anticancer agents on HepG2 cell line with IC50 values of (5.6 ± 0.5 µm) and (29.6 ± 7.6 µm) respectively, and on MCF-7 with IC50 values of (32.1 ± 5.6 µm) and (46.2 ± 8.2 µm) respectively. The molecular docking of compounds 7 and 10 has been studied, and the results reveal that the newly designed piperazine-tagged imidazole derivatives bind to the hydrophobic pocket and polar contact with high affinity.

scholarly journals Synthesis and screening of anticancer potentials of some new terephthaldehyde-derived nitrone compounds

2020 ◽  
Vol 19 (2) ◽  
pp. 341-349
Author(s):  
Husam Hamza Salman ◽  
Munther Abduljaleel Mohammed Ali ◽  
Eman Tariq Ali
Keyword(s):  
Anticancer Agents ◽  
Human Cancer ◽  
Condensation Reaction ◽  
Human Cancer Cell Lines ◽  
Human Cancer Cells ◽  
Anticancer Properties ◽  
Chemical Structures ◽  
Ic50 Values ◽  
Mcf 7

Purpose: To synthesize and screen some new nitrone compounds derived from terephthaldehyde for their anticancer potential. Methods: Six new compounds (H, p-Me,p-Br, p-Cl, o-Cl and m-Me) were synthesized via a condensation reaction between terephthaldehyde and a variety of aryl hydroxylamine compounds derived from nitrobenzene and its derivatives. The chemical structures of these compounds were identified using elemental CHN analysis and were elucidated using Fourier Transform infra-red (FT-IR), 1H-nuclear magnetic resonance (1H NMR), mass spectrometry (MS), and elemental analysis. The anticancer effects of the compounds were screened in vitro with respect to their cytotoxicity on MCF7 human cancer cells line. The IC50 values were obtained by MTT assay and their effects on apoptosis of MCF-7 cells were assessed using Acridine orange-ethidium bromide AO/EtBr staining method under a fluorescence microscope. Results: Only four compounds (2b, 2d, 2e, and 2f) inhibited more than 50 % of the growth of MCF-7 cells. The strongest anti-proliferation effect against MCF-7 cells was exhibited by 2f (m-Me), producing more apoptosis which increased membrane disruption and consistency of lysosome vacuoles; it also exhibited higher cytotoxic effects on human cancer cell lines (IC50 < 7.5) than the other synthesized compounds. Conclusion: The new nitrone compounds (2b, 2d, 2e, and 2f) synthesized from terephthaldehyde exhibit some anticancer properties, and so are potential anticancer agents. Keywords: Terephthaldehyde, Nitrone, Cytotoxicity, Anticancer, MCF-7 cells

scholarly journals New Cytotoxic Natural Products from the Red Sea Sponge Stylissa carteri

Marine Drugs ◽  
2020 ◽  
Vol 18 (5) ◽  
pp. 241 ◽  
Author(s):  
Reda F. A. Abdelhameed ◽  
Eman S. Habib ◽  
Nermeen A. Eltahawy ◽  
Hashim A. Hassanean ◽  
Amany K. Ibrahim ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Red Sea ◽  
Anticancer Agents ◽  
Human Cancer ◽  
Spectroscopic Techniques ◽  
Standard Drug ◽  
Human Cancer Cell Lines ◽  
Stylissa Carteri ◽  
Mcf 7

Bioactivity-guided isolation supported by LC-HRESIMS metabolic profiling led to the isolation of two new compounds, a ceramide, stylissamide A (1), and a cerebroside, stylissoside A (2), from the methanol extract of the Red Sea sponge Stylissa carteri. Structure elucidation was achieved using spectroscopic techniques, including 1D and 2D NMR and HRMS. The bioactive extract’s metabolomic profiling showed the existence of various secondary metabolites, mainly oleanane-type saponins, phenolic diterpenes, and lupane triterpenes. The in vitro cytotoxic activity of the isolated compounds was tested against two human cancer cell lines, MCF-7 and HepG2. Both compounds, 1 and 2, displayed strong cytotoxicity against the MCF-7 cell line, with IC50 values at 21.1 ± 0.17 µM and 27.5 ± 0.18 µM, respectively. They likewise showed a promising activity against HepG2 with IC50 at 36.8 ± 0.16 µM for 1 and IC50 30.5 ± 0.23 µM for 2 compared to the standard drug cisplatin. Molecular docking experiments showed that 1 and 2 displayed high affinity to the SET protein and to inhibitor 2 of protein phosphatase 2A (I2PP2A), which could be a possible mechanism for their cytotoxic activity. This paper spreads light on the role of these metabolites in holding fouling organisms away from the outer surface of the sponge, and the potential use of these defensive molecules in the production of novel anticancer agents.

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