scholarly journals Synthesis of new 3-(substituted-phenyl)-N-(2-hydroxy-2-(substituted-phenyl)ethyl)-N-methylthiophene-2-sulfonamide derivatives as antiproliferative agents

2018 ◽  
Vol 9 (1) ◽  
pp. 13-21 ◽  
Author(s):  
Chandrakant Pawar ◽  
Dattatraya Pansare ◽  
Devanand Shinde
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
1H Nmr ◽  
13C Nmr ◽  
Antiproliferative Activity ◽  
Positive Control ◽  
Antiproliferative Agents ◽  
Ic50 Values ◽  
Mcf 7

In the present work, we report the synthesis of a series of 3-(substituted phenyl)-N-(2-hydroxy-2-(substituted-phenyl)ethyl)-N-methylthiophene-2-sulfonamide derivatives through Suzuki and Buchwald reaction. We have optimized methodology for targets from milligram to multi-gram scale. The newly synthesized compounds were characterized by 1H NMR, 19F NMR, 13C NMR, LC-MS techniques and purity was further checked by HPLC. The compounds were evaluated for their in-vitro antiproliferative activity against MCF-7, HeLa, A-549 and Du-145 cancer cell lines by CCK-8 assay. The preliminary bioassay suggests that most of the compounds show antiproliferation with different degrees and 5-fluorouracil was used as positive control. Among these compounds 2d, 2g, 2i, 4e, 4h and 4k are most active compared to the standard. All the synthesized compounds show IC50 values from 1.82-9.52 µM in different cell lines. Amongst these, compounds 2d, 2g, 2i, 4e, 4h and 4k were most potent, with IC50 values ranging from 1.82-4.28 µM in different cell lines.

scholarly journals In vitro antiproliferative activity of some fluoro-substituted benzimidazole-based scaffolds

2021 ◽  
Vol 4 (1) ◽  
pp. 10-17
Author(s):  
Ronak Haj Ersan ◽  
Nizami Duran
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Mtt Assay ◽  
Antiproliferative Activity ◽  
Cancer Cell Lines ◽  
Positive Control ◽  
Human Cells ◽  
Benzimidazole Derivatives ◽  
Antiproliferative Agents

In the present work, a series of fluoro-substituted benzimidazole derivatives were designed and synthesized as antiproliferative agents. The antiproliferative activity of these compounds was investigated using MTT assay. Fluoro-substituted benzimidazole derivatives showed significant antiproliferative activity against all the tested cancer cell lines. All the derivatives were found to be less toxic as compared to methotrexate (positive control) in human cells, indicating selective and efficient antiproliferative activity of these benzimidazole derivatives. These findings suggest that compounds ORT14 and ORT15 among this series are most effective and have potential for detailed investigations.

scholarly journals Synthesis and Antiproliferative activity in vitro of Amidino Substituted 2-phenylbenzazoles

2019 ◽  
Vol 92 (2) ◽  
pp. 181-189 ◽  
Author(s):  
Livio Racané ◽  
Kristina Butković ◽  
Irena Martin-Kleiner ◽  
Marijeta Kralj ◽  
Grace Karminski-Zamola ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Antiproliferative Activity ◽  
Cancer Cell Lines ◽  
Benzimidazole Derivatives ◽  
Antiproliferative Agents ◽  
Benzothiazole Derivatives

Within this work we describe the synthesis of versatile substituted 2-phenyl benzothiazole 3–10 and 2-phenylbenzimidazole 12–19 derivatives bearing amidino groups. Furthermore, the synthesized compounds were explored for their antiproliferative activity in vitro on three cancer cell lines. Tested compounds showed moderate to strong antiproliferative activity. Furthermore, the type of the attached amidino group on benzazole nuclei has the significant impact on the antiproliferative activity only within benzimidazole derivatives with 2-imidazolinyl substituted derivatives being more active in comparison to amidino substituted analogues. All obtained results revealed that this type of benzothiazole derivatives have a great potential for further optimization and development of more efficient potential antiproliferative agents.

scholarly journals NEW QUINAZOLINONE DERIVATIVES: SYTHESIS AND IN VITRO CYTOTOXIC ACTIVITY

2020 ◽  
Vol 58 (1) ◽  
pp. 12
Author(s):  
Tran Khac Vu
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cytotoxic Effect ◽  
Cancer Cell Lines ◽  
Ic50 Values ◽  
Quinazolinone Derivatives ◽  
Bioassay Result ◽  
Mcf 7

The paper presents a simple synthesis of new quinazolinone derivatives 13a-i. Synthesized derivatives were tested for their cytotoxic effect against three cancer cell lines including SKLU-1, MCF-7 and HepG-2. The bioassay result showed that only compound 13e exhibited significant cytotoxic effect against cancer cell lines tested with IC50 values of 9.48, 20.39 and 18.04 µg/ mL, respectively.

Guanidinyl and Amide Conjugated Benzothiazoles as Potential Anti- Tubercular Agent and their Cytotoxicity Study

2018 ◽  
Vol 16 (2) ◽  
pp. 121-128
Author(s):  
Mahesh Bhat ◽  
S.L. Belagali
Keyword(s):  
Molecular Docking ◽  
Cell Lines ◽  
Positive Control ◽  
Docking Studies ◽  
Benzothiazole Derivatives ◽  
Excellent Activity ◽  
Ic50 Values ◽  
Tuberculosis Activity ◽  
Mcf 7

Background: Two series of Guanidinyl benzothiazole and benzothiazole diamide derivatives were synthesized and screened for their anti-mycobacterial activity and cytotoxicity on cancer cell lines. Methods: The anti-mycobacterium study indicates that all the synthesized benzothiazole compounds were appreciably active and some of the compounds have MIC values lower than the standard drugs. Benzothiazoleguanidinyl derivatives (13a, 13b and 13f) showed the excellent activity with MIC values 1.6 µg/mL. The guanidinyl group and electron donating group present in the molecule interacts with the microorganism and arrest the further growth, indicating excellent activity by these compounds. These benzothiazole derivatives were also tested for cytotoxicity against MCF-7 and KB Mouth cell lines by MTT assay and they were found to be moderately active. Results: For the KB-Mouth cell lines, diamide compounds (9a-9h) have remarkable activity and they showed IC50 values at 10 µg/mL. Compared to benzothiazole diamides, Benzothiazole guanidinyl compounds selectively acted as a good anti-mycobacterium agent. Conclusion: In order to rationalize the in-vitro anti-tuberculosis activity, we carried out molecular docking studies with enoyl acyl carrier reductase (InhA) of M. tuberculosis and they exhibited remarkable docking scores from -5.85 to -9.27, which was comparable with the positive control Isoniazid (INH) with -6.61 as the docking score and showed less affinity towards the DprE1 protiens.

scholarly journals EVALUATION OF ANTIPROLIFERATIVE ACTIVITY OF SIDDHA ANTI-PSORIATIC FORMULATION PANCHAMUGA CHENDHURAM USING CULTURED HUMAN KERATINOCYTE CELL LINES

2019 ◽  
pp. 280-283
Author(s):  
RAJALAKSHMI S ◽  
RAMYA VT ◽  
SAMRAJ K
Keyword(s):  
Cell Lines ◽  
Antiproliferative Activity ◽  
Hacat Cell ◽  
Scientific Evidence ◽  
Positive Control ◽  
Traditional Use ◽  
Human Keratinocyte ◽  
Ic50 Values ◽  
Hacat Cell Lines

Objectives: This study was aimed at scientifically evaluating the in vitro antipsoriatic activity of Siddha drug Panchamuga Chendhuram (PMC) in human keratinocyte (HacaT) cell lines. Methods: The Siddha drug PMC tested for antipsoriatic activity on HacaT cell lines was morphologically examined by phase contrast microscopy, and the cell viability was determined by 3- (4, 5 dimethyl thiazole-2 yl) -2.5-diphenyl tetrazolium bromide assay. About 100 μl of different concentrations (2, 6, 10, 20, 30, 40, 50, 60, 70, 80, 90, and 100 μg/ml) of the test samples were prepared in the cell culture medium and incubated for 24 h and 48 h to determine the viable cells. Results: The results revealed that Siddha drug PMC showed hopeful antiproliferative activity. In vitro studies showed that after 24 h and 48 h incubation, the inhibitory concentration 50 (IC50) values of PMC (IC50 20 μg/ml) were 72.08±27.56 μg/ml and 43.91±17.71 μg/ml, respectively, as compared with Asiaticoside as a positive control with an IC50 value of 20.13 μg/ml. Conclusion: Thus, this study provides scientific evidence about the efficacy of the Siddha drug PMC against the HacaT cell lines confirming its traditional use in psoriasis treatment and also emphasizes the need for antipsoriatic evaluation in animal models.

scholarly journals Synthesis and Biological Evaluation of Novel Isoxazole-Amide Analogues as Anticancer and Antioxidant Agents

2021 ◽  
Vol 2021 ◽  
pp. 1-9
Author(s):  
Ahmad M. Eid ◽  
Mohammed Hawash ◽  
Johnny Amer ◽  
Abdullah Jarrar ◽  
Samira Qadri ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Positive Control ◽  
Biological Evaluation ◽  
Antioxidant Agents ◽  
M Phase ◽  
Ic50 Values ◽  
Causes Of Mortality ◽  
Mcf 7

Cancer now is one of the leading causes of mortality in the world. There has been a lot of effort to discover new anticarcinogenic agents that allow treatment with fewer side effects. A series of isoxazole-carboxamide derivatives (2a–2g) were synthesised and evaluated for their cytotoxic activity against breast (MCF-7), cervical (HeLa), and liver (Hep3B) cancer cell lines and their antioxidant activity in the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. The results showed that 2d and 2e were the most active compounds against Hep3B cells, with a half-maximal inhibitory concentration (IC50) of around 23 μg/ml; 2d showed the highest activity against HeLa cells, with an IC50 15.48 μg/ml. However, 2a had the lowest IC50 (39.80 μg/ml) against MCF-7 cells. By contrast, compound 2g was inactive against all cancer cell lines, with IC50 values >400 μg/ml. Both 2d and 2e reduced Hep3B secretion of alpha-fetoprotein (to 1829.33 ± 65.91   ng / ml and 1758.66 ± 54.04   ng / ml , respectively). Furthermore, in cell cycle analysis, 2d and 2e induced a delay in the G2/M phase of 18.07%, which is similar to the doxorubicin positive control. Moreover, 2d and 2e reduced the necrosis rate of Hep3B threefold and instead shifted the cells to apoptosis. Our results indicate that 2d and 2e have potent and promising anticancer activity. However, compound 2a was the most active as antioxidant agent ( I C 50 = 7.8 ± 1.21   μ g / ml ) compared with Trolox as a positive control (IC50 2.75 μg/ml).

Design, Synthesis and In vitro Cytotoxic Evaluation of Novel Hybrids of Artemisinin and Quinazolinone

2021 ◽  
Vol 18 ◽  
Author(s):  
Tran Khac Vu ◽  
Bach Xuan Nguyen ◽  
Linh Nguyen Pham Duy ◽  
Thuc Bao Nguyen Truong ◽  
Anh Tuan Phung ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Anti Cancer ◽  
Ic50 Values ◽  
Mcf 7

Background: In this study, two novel hybrid series of artemisinin and quinazolinones were synthesized and evaluated in vitro cytotoxicity against two human cancer cell lines, including SKLu-1 (lung cancer), MCF- 7 (breast cancer). The bio-assay results indicated that most of the target compounds exhibited cytotoxic activities against both human cancer cell lines tested, and seemed to be more cytotoxic toward the breast (MCF-7) cancer cells than lung (SKLu-1) cancer cells. Among the synthesized artemisinin hybrids, the compound 13d containing a quinazolinone conjugated system exhibited the most potent cytotoxicity against the SKLu-1 and MCF-7 cell lines with IC50 values of 1.62 and 0.77 µM, respectively. Objective: This study aims at developing novel hybrids of artemisinin and quinazolinones as anti-cancer agents. Method: A series of novel hybrids were designed, synthesized and evaluated for cytotoxicity against two human cancer cell lines, including SKLu-1 and MCF-7 using SRB method. Results : All thirteen hybrids of artemisinin with quinazolinone exhibited cytotoxic activity against two tested cancer cell lines, in which the compound 13d exhibited the most potent cytotoxicity against the SKLu-1 and MCF-7 cell lines with IC50 values of 1.62 and 0.77 µM, respectively. Conclusion: The research results suggest that some compounds could be considered as leads for future design of hybrids and have the potential for further studies in the field of anti-cancer agent development.

scholarly journals Cytostatic Effects of Methanolic Extracts of Amsonia orientalis Decne. on MCF-7 and DU145 Cancer Cell Lines

2017 ◽  
Vol 45 (1) ◽  
pp. 36-42
Author(s):  
Arda ACEMİ ◽  
Gokhan DURUKSU ◽  
Fazıl ÖZEN
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Leaf Extract ◽  
Cancer Cell Lines ◽  
Methanolic Extracts ◽  
Cellular Analysis ◽  
Anti Cancer ◽  
Ic50 Values ◽  
Mcf 7

Amsonia orientalis is an ornamental plant with anti-cancer properties. To characterize the anti-cancer potential of the species, methanolic extracts were prepared from leaf and stem tissues of field-grown individuals. Also, a mixture of stems, leaves and roots of in vitro grown plantlets (SLR) were extracted with methanol and used. Effects of these extracts on the cancer cell lines MCF-7 (breast) and DU145 (prostate) were investigated. After incubation for 48 h, the leaf extract gave the lowest IC50 values (197.8 µM for MCF-7 and 300.9 µM for DU145). The SLR extract also gave the similar results, but with higher IC50 values. The stem extract had the weakest effect on cancer-cell-specific cytotoxicity. The extracts did not have a significant effect on DU145, compared to fibroblasts. The leaf extract increased the number of active-Caspase-3 positive cells in MCF-7 culture slightly, but the main effect of all extracts was on the cell proliferation rather than apoptosis. Real-time cellular analysis of MCF-7 demonstrated a 1.8-fold increase of doubling time for the leaf extract. The expression of proliferation-related gene MCM2 was found to be decreased in MCF-7 cells treated with the leaf extract, while its expression increased in fibroblasts after the same treatment. In conclusion, the extracts affected the MCF-7 cells at moderate concentrations. This study suggests that the leaf methanolic extracts might be a good source of compounds with cytostatical properties.

scholarly journals Synthesis and In vitro Cytotocxic Evaluation of New Quinazolinone Derivatives

2020 ◽  
Vol 36 (3) ◽  
Author(s):  
Tran Dang Thinh ◽  
Tran Khac Vu
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
High Yield ◽  
Ic50 Values ◽  
Hydroxyanthranilic Acid ◽  
Quinazolinone Derivatives ◽  
Bioassay Result ◽  
Mcf 7

The paper presents a simple and efficient synthesis of a series of new quinazolinone derivatives 8a-h. First, the reaction of 5-hydroxyanthranilic acid (6) with acetic anhydride at 160–180oC for 2 h gave the intermediate 7 in high yield. This intermediate was then reacted with amines in acetic acid at 180 oC for 14 h afforded new quinazolinone derivatives 8a-h in 77–92%. Synthesized compounds were structurally confirmed using spectroscopic methods: 1H, 13CNMR and mass spectrum. The bioassay result using three cancer cell lines including SKLU-1 (lung cancer), MCF-7 (breast cancer) and HepG-2 (liver cancer) showed that only compound 8h exhibited significant cytotoxic effect against cancer cell lines tested with IC50 values of 23.09, 27.75 and 30.19 µg/ mL, respectively.

Benzimidazole Derivatives as Potential Antimicrobial and Antiulcer Agents: A Mini Review

2019 ◽  
Vol 19 (16) ◽  
pp. 1292-1297 ◽  
Author(s):  
Ali Mohd Ganie ◽  
Ayaz Mahmood Dar ◽  
Fairooz Ahmad Khan ◽  
Bashir Ahmad Dar
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
1H Nmr ◽  
13C Nmr ◽  
Benzimidazole Derivatives ◽  
Spectroscopic Techniques ◽  
One Pot ◽  
Biological Screening ◽  
Elemental Analyses ◽  
Characterization Studies

:Here in we report the number of strategies for the synthesis of differently substituted benzimidazole derivatives. The protocols involved in the syntheses of these derivatives were one-pot or multi-component. The characterization studies of these derivatives were carried by using different spectroscopic techniques (1H NMR, 13C NMR and MS) and elemental analyses. The biological screening studies revealed that these benzimidazole derivatives show potential antibacterial as well as antifungal behavior. These benzimidazole derivatives not only depicted potential antiulcer properties but also showed moderate to good anticancer/cytotoxic behavior against different cancer cell lines.

Sign in / Sign up

Export Citation Format

Share Document