Thiazole Containing Heterocycles with CNS Activity

Agarwal, Shikha; Kalal, Priyanka; Gandhi, Divyani; Prajapat, Prakash

doi:10.2174/1570163814666170724170152

Cited by 22 publications

(13 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…For example, thiazoles demonstrated antimicrobial, antiviral, anti-diabetic, diuretic, anticonvulsant, antioxidant, anti-HIV, analgesic, anti-inflammatory, neuroprotective, and antitumor activities. These wide and potent activities were extensively published in several review articles (Siddiqui et al, 2011;Leoni et al, 2014;Ayati et al, 2015;Morigi et al, 2015;Rouf and Tanyeli, 2015;Chhabria et al, 2016;Das et al, 2016;Kumar et al, 2016;Agarwal et al, 2018;Scarim et al, 2019;de Oliveira et al, 2020). The anti-cancer activities of thiazole derivatives were also intensively reviewed (Ayati et al, 2019;Sharma et al, 2020).…”

Section: Introductionmentioning

confidence: 99%

Novel Bis-Thiazole Derivatives: Synthesis and Potential Cytotoxic Activity Through Apoptosis With Molecular Docking Approaches

et al. 2021

View full text Add to dashboard Cite

A series of bis-thiazoles 5a–g were synthesized from bis-thiosemicarbazone 3 with hydrazonoyl chlorides 4a–g. Reaction of 3 with two equivalents of α-halocarbonyl compounds 6–8, 10, and 12a–d afforded the corresponding bis-thiazolidines 9, 11, and 13a–d, respectively. Condensation of bis-thiazolidin-4-one 9 with different aromatic aldehydes furnished bis-thiazolidin-4-ones 14a–d. Compounds 5a–g, 9, and 13a,c,d were screened in vitro for their cytotoxic activities in a panel of cancer cell lines. Compounds 5a–c, 5f–g, and 9 exhibited remarkable cytotoxic activities, especially compound 5c with potent IC50 value 0.6 nM (against cervical cancer, Hela cell line) and compound 5f with high IC50 value 6 nM (against ovarian cancer, KF-28 cell line). Compound 5f–induced appreciated apoptotic cell death was measured as 82.76% associated with cell cycle arrest at the G1 phase. The apoptotic pathways activated in KF-28 cells treated with 5a, 5b, and 5f were further investigated. The upregulation of some pro-apoptotic genes, bax and puma, and the downregulation of some anti-apoptotic genes including the Bcl-2 gene were observed, indicating activation of the mitochondrial-dependent apoptosis. Together with the molecular docking studies of compounds 5a and 5b, our data revealed potential Pim-1 kinase inhibition through their high binding affinities indicated by inhibition of phosphorylated C-myc as a downstream target for Pim-1 kinase. Our study introduces a set of bis-thiazoles with potent anti-cancer activities, in vitro.

show abstract

Section: Introductionmentioning

confidence: 99%

Novel Bis-Thiazole Derivatives: Synthesis and Potential Cytotoxic Activity Through Apoptosis With Molecular Docking Approaches

et al. 2021

View full text Add to dashboard Cite

show abstract

“…[1][2][3][4][5][6][7][8][9][10] Some thiazole containing compounds are well established as medicines (Figure 1). [11][12][13][14][15][16] Moreover, among different heterocyclic compounds, benzofuran constitutes the most important class of fused ring heterocyclic. They are considered the core of several interesting pharmacologically active natural products.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of novel bis- and poly(hydrazinylthiazole) linked to benzofuran or benzothiazole as new hybrid molecules

Salem¹,

Darweesh²,

Shaaban³

et al. 2019

Arkivoc

View full text Add to dashboard Cite

show abstract

“…Nitrogen-containing heterocycles specially azoles family are the subject of continuous interest in organic synthesis owing to the fact that they occur ubiquitously in pharmacologically active natural products, multipurpose oriented functional materials as well as highly potent pharmaceuticals and agrochemicals [3,4]. Benzothiazoles found to be most interesting biophore in research because it is used as a synthon for the synthesis of bioactive structures [5]. It is present in compounds involved in research aimed at evaluating new products that possess interesting biological activities viz.…”

Section: Introductionmentioning

confidence: 99%

Importance of Benzothiazole Motif in Modern Drug Discovery: Introduction

Prajapat¹

2018

MADD

Self Cite

View full text Add to dashboard Cite

Drug discovery & their progress is major interest and present to the entire scientific community is a distilled version of newer developments in medicinal and pharmaceutical research area. Benzothiazoles are the most significant heterocyclic scaffold, which are widespread and integral feature of a broad range of natural occurring molecules and pharmaceutical agents. It shows a number of pharmacophoric activities, and its derivatives signify a high degree of structural diversity that has proven helpful for explore of newer bioactive agents.

show abstract

Thiazole Containing Heterocycles with CNS Activity

Cited by 22 publications

References 0 publications

Novel Bis-Thiazole Derivatives: Synthesis and Potential Cytotoxic Activity Through Apoptosis With Molecular Docking Approaches

Novel Bis-Thiazole Derivatives: Synthesis and Potential Cytotoxic Activity Through Apoptosis With Molecular Docking Approaches

Synthesis of novel bis- and poly(hydrazinylthiazole) linked to benzofuran or benzothiazole as new hybrid molecules

Importance of Benzothiazole Motif in Modern Drug Discovery: Introduction

Contact Info

Product

Resources

About