Design, Synthesis, Characterization and Computational Evaluation of Novel Isobutychalcones as Cytotoxic Agents: Part-A

Ab, Shaik; Yr, Prasad; Shahanaaz, Shaik

doi:10.20944/preprints201611.0043.v1

Cited by 7 publications

(7 citation statements)

References 18 publications

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“…Encouraged by the data from the literature regarding the anticancer activity of chalcones [132][133][134][135][136], Suma et al [137] designed and synthesized a library of chalcone-linked thiazole-imidazopyridine (87a-j, Figure 34) with the purpose to study their anticancer activity. Compounds were tested on the following four human cancer cell lines MCF-7 (breast carcinoma), A549 (lung carcinoma), DU-145 (prostate carcinoma), and MDA MB- The presence of the bromine and methoxy group was more beneficial for O-noscapine derivatives 86o and 86c compared to N-noscapinoids (86o, 86c).…”

Section: Thiazole Derivatives As Anticancer Agentsmentioning

confidence: 99%

Thiazole Ring—A Biologically Active Scaffold

2021

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Background: Thiazole is a good pharmacophore nucleus due to its various pharmaceutical applications. Its derivatives have a wide range of biological activities such as antioxidant, analgesic, and antimicrobial including antibacterial, antifungal, antimalarial, anticancer, antiallergic, antihypertensive, anti-inflammatory, and antipsychotic. Indeed, the thiazole scaffold is contained in more than 18 FDA-approved drugs as well as in numerous experimental drugs. Objective: To summarize recent literature on the biological activities of thiazole ring-containing compounds Methods: A literature survey regarding the topics from the year 2015 up to now was carried out. Older publications were not included, since they were previously analyzed in available peer reviews. Results: Nearly 124 research articles were found, critically analyzed, and arranged regarding the synthesis and biological activities of thiazoles derivatives in the last 5 years.

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Section: Thiazole Derivatives As Anticancer Agentsmentioning

confidence: 99%

Thiazole Ring—A Biologically Active Scaffold

2021

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“…The in vitro antiproliferative and cytotoxicity of compounds 1 – 20 was evaluated by Mosmann’s MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) assay method, as described in the literature [ 63 , 64 , 65 ] on prostate cancer cell lines (DU-145). In both the assays, the IC 50 values of the tested compounds were compared with the positive control Methotrexate (Mtx).…”

Section: Methodsmentioning

confidence: 99%

Thiazole–Chalcone Hybrids as Prospective Antitubercular and Antiproliferative Agents: Design, Synthesis, Biological, Molecular Docking Studies and In Silico ADME Evaluation

Kasetti

Singhvi

Nagasuri³

et al. 2021

Molecules

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Compounds bearing thiazole and chalcone pharmacophores have been reported to possess excellent antitubercular and anticancer activities. In view of this, we designed, synthesized and characterized a novel series of thiazole−chalcone hybrids (1–20) and further evaluated them for antitubercular and antiproliferative activities by employing standard protocols. Among the twenty compounds, chalcones 12 and 7, containing 2,4-difluorophenyl and 2,4-dichlorophenyl groups, showed potential antitubercular activity higher than the standard pyrazinamide (MIC = 25.34 µM) with MICs of 2.43 and 4.41 µM, respectively. Chalcone 20 containing heteroaryl 2-thiazolyl moiety exhibited promising antiproliferative activity against the prostate cancer cell line (DU-145), higher than the standard methotrexate (IC50 = 11 ± 1 µM) with an IC50 value of 6.86 ± 1 µM. Furthermore, cytotoxicity studies of these compounds against normal human liver cell lines (L02) revealed that the target molecules were comparatively less selective against L02. Additional computational studies using AutoDock predicted the key binding interactions responsible for the activity and the SwissADME tool computed the in silico drug likeliness properties. The lead compounds generated through this study, create a way for the optimization and development of novel drugs against tuberculosis infections and prostate cancer.

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“…In vitro antibacterial and antifungal activities: The antimicrobial activity was performed against two bacterial and two fungal strains by serial tube dilution method and minimum inhibitory concentration (MIC) of all the compounds were determined against the selected microbes. 22,23 The bacterial strains selected for the study were Staphylococcus aureus (NCIM-2063, Sa) and Proteus vulgaris (NCIM-2027, Pv) whereas the fungal strains include Aspergillus niger (ATCC-6275, An) and Candida tropicalis (ATCC-1369, Ca) respectively. Ciprofloxacin and fluconazole were used as positive controls for the antibacterial and antifungal activities respectively.…”

Section: Biological Studiesmentioning

confidence: 99%

Antimicrobial and antitubercular evaluation of some new 5-amino-1,3,4-thiadiazole-2-thiol derived Schiff bases

BABU¹,

I²,

Nagasuri³

et al. 2020

Rev.Roum.Chim.

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In an effort to study the effect of 1,3,4-thidiazole based molecules on bacteria, fungal and tuberculosis species, we synthesized a series of Schiff bases (2a-2m) by reacting a variety of carbonyl compounds with 5-amino-1,3,4- thiadiazole-2-thiol. Molecular structure of these compounds was retrieved by spectral methods and elemental analysis. All these compounds were evaluated for their antibacterial, antifungal and antitubercular activities employing standard biological protocols. The compounds 2m and 2l substituted with the electron withdrawing fluorine and nitro groups showed excellent inhibitory activity against Staphylococcus aureus, Aspergillus niger and Candida tropicalis with an MIC of 8 µg/mL whereas 2i containing the electron releasing dimethylamino group showed potent activity against Proteus vulgaris. Additionally, 2m along with 2j, 2k and 2l also exhibited superior antimycobacterial activity than the standard pyrazinamide. The activity data for these compounds pave the way for the development of new antimicrobial and antitubercular drugs.

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Design, Synthesis, Characterization and Computational Evaluation of Novel Isobutychalcones as Cytotoxic Agents: Part-A

Cited by 7 publications

References 18 publications

Thiazole Ring—A Biologically Active Scaffold

Thiazole Ring—A Biologically Active Scaffold

Thiazole–Chalcone Hybrids as Prospective Antitubercular and Antiproliferative Agents: Design, Synthesis, Biological, Molecular Docking Studies and In Silico ADME Evaluation

Antimicrobial and antitubercular evaluation of some new 5-amino-1,3,4-thiadiazole-2-thiol derived Schiff bases

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