Synthesis and Biological Evaluation of Novelγ-Alkylidene Butenolides

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).

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Anti-Leishmanial and Cytotoxic Activities of a Series of Maleimides: Synthesis, Biological Evaluation and Structure-Activity Relationship

Molecules ◽

10.3390/molecules23112878 ◽

2018 ◽

Vol 23 (11) ◽

pp. 2878 ◽

Cited By ~ 2

Author(s):

Yongxian Fan ◽

Yuele Lu ◽

Xiaolong Chen ◽

Babu Tekwani ◽

Xing-Cong Li ◽

...

Keyword(s):

Amphotericin B ◽

Biological Evaluation ◽

Activity Relationship ◽

Cytotoxic Activities ◽

In Vitro Test ◽

Standard Drug ◽

Sar Studies ◽

Vitro Test ◽

Better Than

In the present study, 45 maleimides have been synthesized and evaluated for anti-leishmanial activities against L. donovani in vitro and cytotoxicity toward THP1 cells. All compounds exhibited obvious anti-leishmanial activities. Among the tested compounds, there were 10 maleimides with superior anti-leishmanial activities to standard drug amphotericin B, and 32 maleimides with superior anti-leishmanial activities to standard drug pentamidine, especially compounds 16 (IC50 < 0.0128 μg/mL) and 42 (IC50 < 0.0128 μg/mL), which showed extraordinary efficacy in an in vitro test and low cytotoxicities (CC50 > 10 μg/mL). The anti-leishmanial activities of 16 and 42 were 10 times better than that of amphotericin B. The structure and activity relationship (SAR) studies revealed that 3,4-non-substituted maleimides displayed the strongest anti-leishmanial activities compared to those for 3-methyl-maleimides and 3,4-dichloro-maleimides. 3,4-dichloro-maleimides were the least cytotoxic compared to 3-methyl-maleimides and 3,4-non-substituted maleimides. The results show that several of the reported compounds are promising leads for potential anti-leishmanial drug development.

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

MedChemComm ◽

10.1039/c4md00098f ◽

2014 ◽

Vol 5 (7) ◽

pp. 953-957 ◽

Cited By ~ 13

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%.

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

Molecules ◽

10.3390/molecules24030539 ◽

2019 ◽

Vol 24 (3) ◽

pp. 539 ◽

Cited By ~ 7

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.

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

MedChemComm ◽

10.1039/c5md00312a ◽

2015 ◽

Vol 6 (12) ◽

pp. 2170-2174 ◽

Cited By ~ 10

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.

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Synthesis and Biological Evaluation of 6-Substituted Mangiferin Derivatives as Antioxidant and Anticancer agents

Letters in Organic Chemistry ◽

10.2174/1570178618666210813123545 ◽

2021 ◽

Vol 18 ◽

Author(s):

Mohan H. Patil ◽

Uma D. Kabra ◽

Krishna R. Gupta ◽

Milind J. Umekar

Keyword(s):

Antioxidant Activity ◽

Anticancer Agents ◽

Biological Evaluation ◽

Anticancer Activities ◽

Standard Drug ◽

Chemical Structures ◽

Synthesis And Biological Evaluation ◽

Derivatives Of ◽

Better Than

: Esterified and alkyl amine derivatives of mangiferin were synthesized and evaluated for in vitro antioxidant and anticancer activities. The chemical structures of the derivatives were confirmed using elemental analysis and spectral data.The antioxidant activity was assessed using 2,2-diphenyl-1-picrylhydrazy (DPHH) assay and some derivatives displayed antioxidant activity better than mangiferin and standard drug ascorbic acid. Among the synthesized derivatives, few exhibited enhanced anticancer activity against human breast (MDA-MB-231) cancer cell lines, then the parent mangiferin.

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Bis-thiobarbiturates as Promising Xanthine Oxidase Inhibitors: Synthesis and Biological Evaluation

Biomedicines ◽

10.3390/biomedicines9101443 ◽

2021 ◽

Vol 9 (10) ◽

pp. 1443

Author(s):

João L. Serrano ◽

Diana Lopes ◽

Melani J. A. Reis ◽

Renato E. F. Boto ◽

Samuel Silvestre ◽

...

Keyword(s):

Xanthine Oxidase ◽

Biological Activities ◽

Chemical Change ◽

Biological Evaluation ◽

Reference Drug ◽

Xanthine Oxidase Inhibitors ◽

Low Cytotoxicity ◽

Synthesis And Biological Evaluation ◽

Better Than

Xanthine oxidase (XO) is the enzyme responsible for the conversion of endogenous purines into uric acid. Therefore, this enzyme has been associated with pathological conditions caused by hyperuricemia, such as the disease commonly known as gout. Barbiturates and their congeners thiobarbiturates represent a class of heterocyclic drugs capable of influencing neurotransmission. However, in recent years a very large group of potential pharmaceutical and medicinal applications have been related to their structure. This great diversity of biological activities is directly linked to the enormous opportunities found for chemical change off the back of these findings. With this in mind, sixteen bis-thiobarbiturates were synthesized in moderate to excellent reactional yields, and their antioxidant, anti-proliferative, and XO inhibitory activity were evaluated. In general, all bis-thiobarbiturates present a good antioxidant performance and an excellent ability to inhibit XO at a concentration of 30 µM, eight of them are superior to those observed with the reference drug allopurinol (Allo), nevertheless they were not as effective as febuxostat. The most powerful bis-thiobarbiturate within this set showed in vitro IC50 of 1.79 μM, which was about ten-fold better than Allo inhibition, together with suitable low cytotoxicity. In silico molecular properties such as drug-likeness, pharmacokinetics, and toxicity of this promising barbiturate were also analyzed and herein discussed.

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

Current Drug Discovery Technologies ◽

10.2174/1570163816666190411110331 ◽

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.

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Synthesis and biological evaluation of some novel pyrazolopyrimidines incorporating a benzothiazole ring system

Acta Pharmaceutica ◽

10.2478/acph-2013-0001 ◽

2013 ◽

Vol 63 (1) ◽

pp. 19-30 ◽

Cited By ~ 11

Author(s):

Mohammed Afzal Azam ◽

Loganathan Dharanya ◽

Charu Chandrakant Mehta ◽

Sumit Sachdeva

Keyword(s):

Antimicrobial Activity ◽

Diclofenac Sodium ◽

Biological Evaluation ◽

Ring System ◽

Standard Drug ◽

Anti Inflammatory ◽

Pyrimidine Moiety ◽

Synthesis And Biological Evaluation

In the present study, a series of benzothiazol derivatives 3a-l containing pyrazolo[3,4-d]pyrimidine moiety at the second position were synthesized and characterized by analytical and spectral data. The compounds were tested for their in vitro antimicrobial activity. Compounds 1-(1,3-benzothiazol-2- yl)-3-methyl-4-phenyl-1H-pyrazolo[3,4-d]pyrimidine (3a), 1- (1,3-benzothiazol-2-yl)-4-(4-chlorophenyl)-3-methyl-1H-pyrazolo[ 3,4-d]pyrimidine (3d) and 1-(1,3-benzothiazol-2-yl)- 3-methyl-4-substituted phenyl-1H-pyrazolo[3,4-d]pyrimidines (3h-j) showed significant inhibitory activity against P. aeruginosa whereas compounds 1-(1,3-benzothiazol-2-yl)-4- (2-chlorophenyl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3b), 2-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin- 4-yl]phenol (3e), 1-(1,3-benzothiazol-2-yl)-4-(3,4-dimethoxyphenyl)- 3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3h), 4-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyri midin-4-yl]-N,N-dimethylaniline (3j) and 1-(1,3-benzothiazol- 2-yl)-3-methyl-4-[2-phenylvinyl]-1H-pyrazolo[3,4-d]pyrimidine (3k) were found to be active against C. albicans. Some of these synthesized compounds were evaluated for their in vivo acute toxicity, analgesic, anti-inflammatory, and ulcerogenic actions. The tested compound 4-[1-(1,3-benzothiazol- 2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-4-yl]-N, N-dimethylaniline (3j) exhibited maximum analgesic and anti-inflammatory activities. Compounds 1-(1,3-benzothiazol- -2-yl)-3-methyl-4-(3-nitrophenyl)-1H-pyrazolo[3,4-d]pyrimidine (3i) and 3j showed a significant gastrointestinal protection compared to the standard drug diclofenac sodium.

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