Design, Synthesis and in vitro Cytotoxicity Evaluation of New Fluorinated Ionic Salt
(S)-(+)-2,3-Dihydro-1H-pyrrolo[2,1-c][1,4]benzodiazepine-5,11(10H,11aH)-dione as
Strategies for Improving Anticonvulsant Activity

The reaction of (S)-(+)-2,3-dihydro-1H-pyrrolo[2,1-c][1,4]benzodiazepine-5,11(10H,11aH)-dione (1) with 4-(trifluoromethyl)benzoic acid (2, C8H5F3O2) in dimethylformamide leads to the formation of C8H5F3O2 (1) as a classical ionic salt 3. The structure of new compound has been characterized by FTIR, 1H NMR, 13C NMR, HRMS spectroscopy. The new compound was tested for in vitro cytotoxicity evaluation by MTT assay against breast adenocarcinoma cell line of MCF-7 cells. A new compound 3 (IC50:199 μM) emerged as minimal toxic when compared to clinical drugs carbamazepine, topiramate and benzodiazepine. A preliminary study of structure activity relationship revealed that the incorporation of fluoro or trifluoromethyl moiety into the compound, even through ionic bond formation, had a great effect on the biological activity and with less toxicity or side effects.

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Anticancer Properties of Safawi Date (Phoenix Dactylifera L.) Seed Extract against Human Breast Adenocarcinoma Cell Line (MCF-7): In-vitro Study

International Journal of Pharmaceutical Research ◽

10.31838/ijpr/2020.12.03.289 ◽

2020 ◽

Vol 12 (03) ◽

Keyword(s):

In Vitro Study ◽

Phoenix Dactylifera ◽

Breast Adenocarcinoma ◽

Human Breast ◽

Adenocarcinoma Cell Line ◽

Anticancer Properties ◽

Human Breast Adenocarcinoma ◽

Phoenix Dactylifera L ◽

Mcf 7

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Evaluation of Cytotoxic and Tyrosinase Inhibitory Activities of 2-phenoxy(thiomethyl) pyridotriazolopyrimidines: In Vitro and Molecular Docking Studies

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520620666200627212128 ◽

2020 ◽

Vol 20 (14) ◽

pp. 1714-1721

Author(s):

Hatem A. Abuelizz ◽

El Hassane Anouar ◽

Mohamed Marzouk ◽

Mizaton H. Hasan ◽

Siti R. Saleh ◽

...

Keyword(s):

Molecular Docking ◽

Kojic Acid ◽

Docking Studies ◽

Breast Adenocarcinoma ◽

Amino Acid Residues ◽

New Class ◽

Structure Activity ◽

Tyrosinase Inhibitors ◽

Mcf 7

Background: The use of tyrosinase has confirmed to be the best means of recognizing safe, effective, and potent tyrosinase inhibitors for whitening skin. Twenty-four 2-phenoxy(thiomethyl)pyridotriazolopyrimidines were synthesized and characterized in our previous studies. Objective: The present work aimed to evaluate their cytotoxicity against HepG2 (hepatocellular carcinoma), A549 (pulmonary adenocarcinoma), MCF-7 (breast adenocarcinoma) and WRL 68 (embryonic liver) cell lines. Methods: MTT assay was employed to investigate the cytotoxicity, and a tyrosinase inhibitor screening kit was used to evaluate the Tyrosinase (TYR) inhibitory activity of the targets. Results: The tested compounds exhibited no considerable cytotoxicity, and nine of them were selected for a tyrosinase inhibitory test. Compounds 2b, 2m, and 5a showed good inhibitory percentages against TYR compared to that of kojic acid (reference substance). Molecular docking was performed to rationalize the Structure-Activity Relationship (SAR) of the target pyridotriazolopyrimidines and analyze the binding between the docked-selected compounds and the amino acid residues in the active site of tyrosinase. Conclusion: The target pyridotriazolopyrimidines were identified as a new class of tyrosinase inhibitors.

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CYTOTOXIC ACTIVITY OF LUVUNGA SCANDENS AGAINST HUMAN CANCER CELL LINES

Jurnal Teknologi ◽

10.11113/jt.v78.7328 ◽

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.

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In vitro cytotoxicity of Strobilanthes crispus ethanol extract on hormone dependent human breast adenocarcinoma MCF-7 cell

BMC Complementary and Alternative Medicine ◽

10.1186/1472-6882-12-35 ◽

2012 ◽

Vol 12 (1) ◽

Cited By ~ 14

Author(s):

Hueh Zan Chong ◽

Asmah Rahmat ◽

Swee Keong Yeap ◽

Abdah Md Akim ◽

Noorjahan Banu Alitheen ◽

...

Keyword(s):

Ethanol Extract ◽

In Vitro Cytotoxicity ◽

Breast Adenocarcinoma ◽

Human Breast ◽

Human Breast Adenocarcinoma ◽

Strobilanthes Crispus ◽

Mcf 7

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Amphiphilic Poly(N-vinylpyrrolidone) Nanoparticles Conjugated with DR5-Specific Antitumor Cytokine DR5-B for Targeted Delivery to Cancer Cells

Pharmaceutics ◽

10.3390/pharmaceutics13091413 ◽

2021 ◽

Vol 13 (9) ◽

pp. 1413

Author(s):

Anne Yagolovich ◽

Andrey Kuskov ◽

Pavel Kulikov ◽

Leily Kurbanova ◽

Dmitry Bagrov ◽

...

Keyword(s):

Drug Delivery ◽

Targeted Delivery ◽

In Vitro Cytotoxicity ◽

Breast Adenocarcinoma ◽

Hydrophobic Core ◽

Tumor Spheroids ◽

Wide Range ◽

Therapeutic Molecules ◽

Mcf 7

Nanoparticles based on the biocompatible amphiphilic poly(N-vinylpyrrolidone) (Amph-PVP) derivatives are promising for drug delivery. Amph-PVPs self-aggregate in aqueous solutions with the formation of micellar nanoscaled structures. Amph-PVP nanoparticles are able to immobilize therapeutic molecules under mild conditions. As is well known, many efforts have been made to exploit the DR5-dependent apoptosis induction for cancer treatment. The aim of the study was to fabricate Amph-PVP-based nanoparticles covalently conjugated with antitumor DR5-specific TRAIL (Tumor necrosis factor-related apoptosis-inducing ligand) variant DR5-B and to evaluate their in vitro cytotoxicity in 3D tumor spheroids. The Amph-PVP nanoparticles were obtained from a 1:1 mixture of unmodified and maleimide-modified polymeric chains, while DR5-B protein was modified by cysteine residue at the N-end for covalent conjugation with Amph-PVP. The nanoparticles were found to enhance cytotoxicity effects compared to those of free DR5-B in both 2D (monolayer culture) and 3D (tumor spheroids) in vitro models. The cytotoxicity of the nanoparticles was investigated in human cell lines, namely breast adenocarcinoma MCF-7 and colorectal carcinomas HCT116 and HT29. Notably, DR5-B conjugation with Amph-PVP nanoparticles sensitized resistant multicellular tumor spheroids from MCF-7 and HT29 cells. Taking into account the nanoparticles loading ability with a wide range of low-molecular-weight antitumor chemotherapeutics into hydrophobic core and feasibility of conjugation with hydrophilic therapeutic molecules by click chemistry, we suggest further development to obtain a versatile system for targeted drug delivery into tumor cells.

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In-vitro cytotoxicity study of methanolic fraction from Ajuga Bracteosa wall ex. benth on MCF-7 breast adenocarcinoma and hep-2 larynx carcinoma cell lines

Pharmacognosy Research ◽

10.4103/0974-8490.122923 ◽

2014 ◽

Vol 6 (1) ◽

pp. 87 ◽

Cited By ~ 6

Author(s):

RajeshS Pawar ◽

FedelicAshish Toppo ◽

Akiriti Pal ◽

PradeepK Chaurasiya ◽

PradeepK Singour

Keyword(s):

Cell Lines ◽

Carcinoma Cell ◽

In Vitro Cytotoxicity ◽

Breast Adenocarcinoma ◽

Larynx Carcinoma ◽

Carcinoma Cell Lines ◽

Mcf 7

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Synthesis, in-vitro cytotoxicity of 1H-benzo[f]chromene derivatives and structure–activity relationships of the 1-aryl group and 9-position

Zeitschrift für Naturforschung C ◽

10.1515/znc-2016-0139 ◽

2017 ◽

Vol 72 (5-6) ◽

pp. 161-171 ◽

Cited By ~ 4

Author(s):

Hany M. Mohamed ◽

Ahmed M. Fouda ◽

Essam S.A.E.H. Khattab ◽

Ahmed M. El- Agrody ◽

Tarek H. Afifi

Keyword(s):

Phenyl Ring ◽

In Vitro Cytotoxicity ◽

Cytotoxic Activities ◽

Specific Group ◽

Aryl Group ◽

Sar Studies ◽

Structure Activity ◽

Hct 116 ◽

Mcf 7

Abstract A series of 1H-benzo[f]chromene-2-carbonitriles was synthesized and evaluated for their cytotoxic activities against MCF-7, HCT-116, and HepG-2 cancer cells. The SAR studies reported that the substitution in the phenyl ring at 1-position of 1H-benzo[f]chromene nucleus with the specific group, H atom, or methoxy group at 9-position increases the ability of the molecule against the different cell lines.

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