Synthesis, &lt;i&gt;in-Vitro&lt;/i&gt; Cytotoxicity and Antimicrobial Evaluations of Some Novel Thiazole Based Heterocycles

In this report, lanthanum strontium manganite at different Sr2+ ion concentrations, as well as Gd3+ or Sm3+ ion substituted La0.5−YMYSr0.5MnO3 (M = Gd and Sm, y = 0.2), have been purposefully tailored using a sol gel auto-combustion approach. XRD profiles confirmed the formation of a monoclinic perovskite phase. FE-SEM analysis displayed a spherical-like structure of the La0.8Sr0.2MnO3 and La0.3Gd0.2Sr0.2MnO3 samples. The particle size of the LSM samples was found to decrease with increased Sr2+ ion concentration. For the first time, different LSM concentrations were inspected for their cytotoxic activity against CACO-2 (intestinal carcinoma cells) and HepG-2 (human hepatocellular carcinoma cells). The cell viability for CACO-2 and HepG-2 was assayed and seen to decrease depending on the Sr2+ ion concentration. Half maximal inhibitory concentration IC50 of CACO-2 cell and HepG-2 cell inhibition was connected with Sr2+ ion ratio. Low IC50 was noticable at low Sr2+ ion content. Such results were correlated to the particle size and the morphology. Indeed, the IC50 of CACO-2 cell inhibition by LSM at a strontium content of 0.2 was 5.63 ± 0.42 µg/mL, and the value increased with increased Sr2+ ion concentration by up to 0.8 to be = 25 ± 2.7 µg/mL. Meanwhile, the IC50 of HepG-2 cell inhibition by LSM at a strontium content of 0.2 was 6.73 ± 0.4 µg/mL, and the value increased with increased Sr2+ ion concentration by up to 0.8 to be 31± 3.1 µg/mL. All LSM samples at different conditions were tested as antimicrobial agents towards fungi, Gram positive bacteria, and Gram negative bacteria. For instance, all LSM samples were found to be active towards Gram negative bacteria Escherichia coli, whereas some samples have presumed antimicrobial effect towards Gram negative bacteria Proteus vulgaris. Such results confirmed that LSM samples possessed cytotoxicity against CACO-2 and HepG-2 cells, and they could be considered to play a substantial role in pharmaceutical and therapeutic applications.

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“…The materials and cell line propagation of CACO-2 and HepG-2 cells have previously been explained in detail [ 25 , 26 ].…”

Section: Methodsmentioning

confidence: 99%

A Robust and Highly Precise Alternative against the Proliferation of Intestinal Carcinoma and Human Hepatocellular Carcinoma Cells Based on Lanthanum Strontium Manganite Nanoparticles

et al. 2021

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“…Antibacterial (against both gram-positive and gram-negative bacteria), antiviral, antifungal, antituberculose, and antiparasitic activity of compounds containing thiazolopyridine structure were reported [247][248][249][250][251]. Additionally, cytotoxic and anticancer activity of thiazolopyridine derivatives were investigated in many studies [252][253][254][255].…”

Section: Thiazolopyridines and Isothiazolopyridinesmentioning

confidence: 99%

Fused Pyridine Derivatives: Synthesis and Biological Activities

Istanbullu¹,

Bayraktar²,

Saylam³

2023

Exploring Chemistry With Pyridine Derivatives

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Five-membered heteroaromatic ring fused pyridine derivatives are of increasing interest in drug design and medicinal chemistry. The structural similarity of many drugs (especially antiviral and anticancer ones) with DNA bases such as adenine and guanine is a key factor to explain their effectiveness. Apart from these, it is also found in the structures of substances with antituberculosis, antibacterial, antifungal, anti-inflammatory, and antimalarial activities. Another advantage of this group of compounds is their positive contribution to solubility, polarity, lipophilicity, and hydrogen bonding capacity properties of the compounds they are incorporated into. In this chapter, various bioactivities of fused pyridine derivatives will be categorized and summarized.

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“…In comparison, El-Mawgoud [34] synthesized some novel 5-[4-(arylmethylideneamino)-1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-ylidene]-2-thioxo-1,3-thiazolidin-4-ones. Compounds…”

Section: -Substituted Rhodanine Derivativesmentioning

confidence: 99%

“…In comparison, El-Mawgoud [34] synthesized some novel 5-[4-(arylmethylideneamino)-1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-ylidene]-2-thioxo-1,3-thiazolidin-4ones. Compounds 14 and 15 and their cytotoxicity against human breast carcinoma cell line were evaluated (Figure 6).…”

Section: -Substituted Rhodanine Derivativesmentioning

confidence: 99%

Anticancer Profile of Rhodanines: Structure–Activity Relationship (SAR) and Molecular Targets—A Review

2022

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The rhodanine core is a well-known privileged heterocycle in medicinal chemistry. The rhodanines, as subtypes of thiazolidin-4-ones, show a broad spectrum of biological activity, including anticancer properties. This review aims to analyze the anticancer features of the rhodanines described over the last decade in the scientific literature. The structure–activity relationship of rhodanine derivatives, as well as some of the molecular targets, were discussed. The information contained in this review could be of benefit to the design of new, effective small molecules with anticancer potential among rhodanine derivatives or their related heterocycles.

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Synthesis, <i>in-Vitro</i> Cytotoxicity and Antimicrobial Evaluations of Some Novel Thiazole Based Heterocycles

Cited by 6 publications

References 42 publications

A Robust and Highly Precise Alternative against the Proliferation of Intestinal Carcinoma and Human Hepatocellular Carcinoma Cells Based on Lanthanum Strontium Manganite Nanoparticles

A Robust and Highly Precise Alternative against the Proliferation of Intestinal Carcinoma and Human Hepatocellular Carcinoma Cells Based on Lanthanum Strontium Manganite Nanoparticles

Fused Pyridine Derivatives: Synthesis and Biological Activities

Anticancer Profile of Rhodanines: Structure–Activity Relationship (SAR) and Molecular Targets—A Review

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