scholarly journals Synthesis and Biological Evaluation of Some Novel Thiazole-Based Heterocycles as Potential Anticancer and Antimicrobial Agents

Molecules ◽  
2019 ◽  
Vol 24 (3) ◽  
pp. 539 ◽  
Author(s):  
Sraa Abu-Melha ◽  
Mastoura Edrees ◽  
Heba Salem ◽  
Nabila Kheder ◽  
Sobhi Gomha ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
Bacterial Species ◽  
Hepatoprotective Activity ◽  
Biological Evaluation ◽  
Cytotoxic Activities ◽  
Thiazole Derivatives ◽  
Biological Assays ◽  
Hct 116 ◽  
Synthesis And Biological Evaluation

A novel series of thiazole-based heterocycles was synthesized using 1,3-dipolar cycloaddition reactions in the presence of chitosan-grafted-poly(vinylpyridine) as an eco-friendly biopolymeric basic catalyst. The molecular structure of the synthesized compounds was illustrated by spectroscopic and elemental analysis. Various in vitro biological assays were performed to explore the potential antitumor, antimicrobial and hepatoprotective activities of the newly synthesized compounds. The cytotoxic activities were assessed against human hepatocellular carcinoma (HepG-2), colorectal carcinoma (HCT-116) and breast cancer (MCF-7) cell lines and results revealed that all compounds displayed antitumor activities with the chlorine-containing derivatives, 11c and 6g, being the most potent. The majority of the tested thiazole derivatives exhibited satisfactory antibacterial activity towards the used gram positive and gram-negative bacterial species. Moreover, many derivatives showed weak hepatoprotective activity against CCl4-induced hepatotoxicity.

Synthesis and biological evaluation of lipid-like 5-(2-hydroxyethyl)-4-methyl-1,3-thiazole derivatives as potential anticancer and antimicrobial agents

MedChemComm ◽  
2015 ◽  
Vol 6 (8) ◽  
pp. 1464-1470 ◽  
Author(s):  
Alla Zablotskaya ◽  
Izolda Segal ◽  
Athina Geronikaki ◽  
Galina Kazachonokh ◽  
Yuris Popelis ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Drug Development ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Thiazole Derivatives ◽  
Synthesis And Biological Evaluation

The observed coupling of high anticancer and antimicrobial activity for novel lipid-like compounds9,10and13based on the 5-(2-hydroxyethyl)-4-methyl-1,3-thiazole scaffold can be important as a basis for further drug development.

Synthesis and biological evaluation of novel bivalent β-carbolines as potential antitumor agents

MedChemComm ◽  
2014 ◽  
Vol 5 (7) ◽  
pp. 953-957 ◽  
Author(s):  
Qifeng Wu ◽  
Zhushuang Bai ◽  
Qin Ma ◽  
Wenxi Fan ◽  
Liang Guo ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Biological Evaluation ◽  
Cytotoxic Activities ◽  
Lewis Lung ◽  
Lewis Lung Cancer ◽  
Synthesis And Biological Evaluation ◽  
Tumor Inhibition Rate ◽  
Potential Antitumor

A series of bivalent β-carbolines with a spacer between the 3-carboxyl oxygens was synthesized and their cytotoxic activities in vitro and antitumor efficacies in vivo were evaluated. Compound 22 exhibited potent antitumor activity against Lewis lung cancer in mice with a tumor inhibition rate of 64.2%.

scholarly journals Synthesis and Biological Evaluation of 1,2,3-Triazole Tethered Thymol-1,3,4-Oxadiazole Derivatives as Anticancer and Antimicrobial Agents

2021 ◽  
Vol 14 (9) ◽  
pp. 866
Author(s):  
Abdulraheem S. A. Almalki ◽  
Syed Nazreen ◽  
Azizah M. Malebari ◽  
Nada M. Ali ◽  
Ahmed A. Elhenawy ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Standard Drug ◽  
E Coli ◽  
Hct 116 ◽  
Oxadiazole Derivatives ◽  
Synthesis And Biological Evaluation ◽  
Better Than ◽  
Mcf 7

A library of 1,2,3-triazole-incorporated thymol-1,3,4-oxadiazole derivatives (6–18) hasbeen synthesized and tested for anticancer and antimicrobial activities. Compounds 7, 8, 9, 10, and 11 exhibited significant antiproliferative activity. Among these active derivatives, compound 2-(4-((5-((2-isopropyl-5-methylphenoxy)methyl)-1,3,4-oxadiazol-2-ylthio)methyl)-1H-1,2,3-triazol-1-yl)phenol (9) was the best compound against all three tested cell lines, MCF-7 (IC50 1.1 μM), HCT-116 (IC50 2.6 μM), and HepG2 (IC50 1.4 μM). Compound 9 was found to be better than the standard drugs, doxorubicin and 5-fluorouracil. These compounds showed anticancer activity through thymidylate synthase inhibition as they displayed significant TS inhibitory activity with IC50 in the range 1.95–4.24 μM, whereas the standard drug, Pemetrexed, showed IC50 7.26 μM. The antimicrobial results showed that some of the compounds (6, 7, 9, 16, and 17) exhibited good inhibition on Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus). The molecular docking and simulation studies supported the anticancer and antimicrobial data. It can be concluded that the synthesized 1,2,3-triazole tethered thymol-1,3,4-oxadiazole conjugates have both antiproliferative and antimicrobial potential.

scholarly journals Synthesis and Biological Evaluation of Novelγ-Alkylidene Butenolides

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Gai-Zhi Liu ◽  
Yan-Bin Guan ◽  
Ya Wu ◽  
Hong-Min Liu
Keyword(s):  
Biological Evaluation ◽  
Cytotoxic Activities ◽  
Test Results ◽  
In Vitro Activity ◽  
Reference Compound ◽  
Activity Test ◽  
Synthesis And Biological Evaluation ◽  
Mic Value ◽  
Better Than

Three new series of 4-substituted-5-alkylidene-2,5-dihydrofuran-2-ones were synthesized. The in vitro activity test results showed that some of them exhibited good antibacterial and cytotoxic activities. Among them compound5cshowed the most potent antibacterial activity againstEscherichia coliwith the MIC value of 20.00 μg/mL. Compound9cshowed good cytotoxic activity against Ec9706 cells withIC50value of 19.39 μM, better than that of the reference compound fluorouracil (IC50=37.74 μM).

Synthesis and biological evaluation of piperazine group-linked bivalent β-carbolines as potential antitumor agents

MedChemComm ◽  
2015 ◽  
Vol 6 (12) ◽  
pp. 2170-2174 ◽  
Author(s):  
Rongqin Sun ◽  
Rui Liu ◽  
Chi Zhou ◽  
Zhenghua Ren ◽  
Liang Guo ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Antitumor Agents ◽  
Biological Evaluation ◽  
Cytotoxic Activities ◽  
Synthesis And Biological Evaluation ◽  
Potential Antitumor

A series of bivalent β-carbolines with a piperazine group spacer between 3-methylene units were synthesized and their cytotoxic activities in vitro were evaluated. Compounds 7e and 7g exhibited potent cytotoxic activity.

scholarly journals Comparative assessment of antimicrobial, antiradical and cytotoxic activities of cannabidiol and its propyl analogue cannabidivarin

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Chiara Russo ◽  
Margherita Lavorgna ◽  
Roberta Nugnes ◽  
Elena Orlo ◽  
Marina Isidori
Keyword(s):  
Cannabis Sativa ◽  
Bacterial Species ◽  
Membrane Damage ◽  
Antibacterial Activities ◽  
Cytotoxic Activities ◽  
Biological Assays ◽  
Plasma Membrane Damage ◽  
Susceptibility Tests ◽  
Human Infections

AbstractCannabidiol and cannabidivarin are phytocannabinoids produced by Cannabis indica and Cannabis sativa. Cannabidiol has been studied more extensively than its propyl analogue cannabidivarin. Therefore, we performed a battery of in vitro biological assays to compare the cytotoxic, antiradical and antibacterial activities of both cannabinoids. Potential mitochondrial metabolism alterations, DNA synthesis inhibition, and plasma membrane damage were studied by MTT assay, BrdU-ELISA and LDH assay of cancer and normal human cells exposed to cannabinoids. ABTS and DPPH assays were performed to observe the effects of the cannabinoids on free radicals. Microbial susceptibility tests were performed to study the activity of the cannabinoids in two bacterial species implicated in human infections, Escherichia coli and Staphylococcus aureus. The results showed that the cannabinoids induced medium levels of cytotoxicity in cancer and normal cells at concentrations ranging from 15.80 to 48.63 and from 31.89 to 151.70 µM, respectively, after 72 h of exposure. Cannabinoids did not exhibit a strong antioxidant capacity in scavenging ABTS or DPPH radicals. No evident differences were observed between the two cannabinoids in antimicrobial activity, except with respect to S. aureus, which showed greater susceptibility to cannabidiol than to cannabidivarin after 72 h of exposure.

scholarly journals Synthesis and Biological Evaluation of Thiazolyl-Ethylidene Hydrazino-Thiazole Derivatives: A Novel Heterocyclic System

2021 ◽  
Vol 11 (19) ◽  
pp. 8908
Author(s):  
Laila A. Al-Mutabagani ◽  
Fathy M. Abdelrazek ◽  
Sobhi M. Gomha ◽  
Ali S. Hebishy ◽  
Mohamed S. Abdelfattah ◽  
...  
Keyword(s):  
Cell Lines ◽  
Biological Evaluation ◽  
Liver Carcinoma ◽  
Cytotoxic Activities ◽  
Thiazole Derivatives ◽  
Reference Drug ◽  
Anticancer Properties ◽  
Breast Carcinoma Cell Lines

The reaction of 2-(1-(2-(2-(4-methoxybenzylidene)hydrazinyl)-4-methylthiazol-5-yl)ethylidene)hydrazinecarbothioamide with a range of hydrazonoyl chlorides and α-halo-compounds yielded three new series of thiazole derivatives. Chemical and physical techniques were used to analyze all newly prepared derivatives (1H-NMR, 13C-NMR, FT-IR and mass spectrometry). The potential antimicrobial and anticancer properties of the synthesized derivatives were investigated using various in vitro biological experiments. Most of the thiazole compounds tested were effective against Gram-positive and Gram-negative bacteria. In addition, a minimum inhibition concentration was determined for the antibiotic properties of the most active produced substances. The cytotoxic activities were tested on HepG-2 (liver carcinoma), HCT-116 (colorectal carcinoma) and MDA-MB-231 (breast carcinoma) cell lines in comparison with cisplatin reference drug and using colorimetric MTT assay. The results detected that compound 10c was the most potent against the three tested cell lines. Interestingly, when the tested compounds were evaluated for their toxicity against normal (MRC-5) cells, they exhibited low toxic effects indicating the safe use of most of them that may require further in vivo and pharmacological studies.

scholarly journals Synthesis and Biological Evaluation of Novel Betulin Derivatives with Aromatic Hydrazone Side Chain as Potential Anticancer Agents

2021 ◽  
Author(s):  
Jiafeng Wang ◽  
Jiale Wu ◽  
Yinglong Han ◽  
Jie Zhang ◽  
Yu Lin ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Antitumor Agents ◽  
Biological Evaluation ◽  
Carcinoma Cells ◽  
Side Chain ◽  
Human Carcinoma ◽  
Hct 116 ◽  
Synthesis And Biological Evaluation ◽  
Mcf 7

A series of novel betulin-28-hydrazone derivatives (7a-7o) were synthesized. All compounds were evaluated for their in vitro cytotoxicities in four human carcinoma cells (HepG2, MCF-7, HCT-116 and A549). Among them, compound 7l displayed the most potent cytotoxicity with an IC50 (concentration of the tested compound that inhibits 50% of cell growth) value of 7.37 ± 0.38 μM against MCF-7 cells. The preliminary cellular mechanism studies indicated that compound 7l could induce MCF-7 cells apoptosis. The above findings indicated that compound 7l may be used as a lead compound for antitumor agents with improved efficacy.

Hybrid Design of Isonicotinic Acid Hydrazide Derivatives: Machine Learning Studies, Synthesis and Biological Evaluation of their Antituberculosis Activity

2020 ◽  
Vol 17 (3) ◽  
pp. 365-375
Author(s):  
Vasyl Kovalishyn ◽  
Diana Hodyna ◽  
Vitaliy O. Sinenko ◽  
Volodymyr Blagodatny ◽  
Ivan Semenyuta ◽  
...  
Keyword(s):  
Machine Learning ◽  
Isonicotinic Acid ◽  
Acid Hydrazide ◽  
Predictive Ability ◽  
Antitubercular Activity ◽  
Biological Evaluation ◽  
Starting Point ◽  
Binary Classifiers ◽  
Synthesis And Biological Evaluation

Background: Tuberculosis (TB) is an infection disease caused by Mycobacterium tuberculosis (Mtb) bacteria. One of the main causes of mortality from TB is the problem of Mtb resistance to known drugs. Objective: The goal of this work is to identify potent small molecule anti-TB agents by machine learning, synthesis and biological evaluation. Methods: The On-line Chemical Database and Modeling Environment (OCHEM) was used to build predictive machine learning models. Seven compounds were synthesized and tested in vitro for their antitubercular activity against H37Rv and resistant Mtb strains. Results: A set of predictive models was built with OCHEM based on a set of previously synthesized isoniazid (INH) derivatives containing a thiazole core and tested against Mtb. The predictive ability of the models was tested by a 5-fold cross-validation, and resulted in balanced accuracies (BA) of 61–78% for the binary classifiers. Test set validation showed that the models could be instrumental in predicting anti- TB activity with a reasonable accuracy (with BA = 67–79 %) within the applicability domain. Seven designed compounds were synthesized and demonstrated activity against both the H37Rv and multidrugresistant (MDR) Mtb strains resistant to rifampicin and isoniazid. According to the acute toxicity evaluation in Daphnia magna neonates, six compounds were classified as moderately toxic (LD50 in the range of 10−100 mg/L) and one as practically harmless (LD50 in the range of 100−1000 mg/L). Conclusion: The newly identified compounds may represent a starting point for further development of therapies against Mtb. The developed models are available online at OCHEM http://ochem.eu/article/11 1066 and can be used to virtually screen for potential compounds with anti-TB activity.

Sign in / Sign up

Export Citation Format

Share Document