Synthesis, structure characterization, in vitro and in silico biological evaluation of a new series of thiazole nucleus integrated with pyrazoline scaffolds

Sadashiva, Rajitha; Naral, Damodara; Kudva, Jyothi; Kumar, Shankar; Byrappa, K.; Shafeeulla, R. Mohammed; Kumsi, Manjunatha

doi:10.1016/j.molstruc.2017.05.066

Cited by 22 publications

(10 citation statements)

References 35 publications

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“…A slightly different approach to thiazole hybrids was followed by Sadashiva et al and by Santosh et al in two recently published articles. The first group synthesized a series of thiazoles linked through a (hydrazino)carbothioamide linker to the pyrazoline [ 116 ]. Among them, compound 48 ( Figure 17 ) showed similar to or better activity than the positive control cisplatin against A549 and MCF-7 cancer cell lines (IC 50 5.0 (10.0) and 7.5 (7.5) μM, respectively—in parentheses is the IC 50 values of cisplatin).…”

Section: 2-pyrazolinesmentioning

confidence: 99%

Pyrazoline Hybrids as Promising Anticancer Agents: An Up-to-Date Overview

Matiadis

Sagnou

2020

IJMS

104

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Pyrazolines are five-membered heterocycles possessing two adjacent nitrogens. They have attracted significant attention from organic and medicinal chemists due to their potent biological activities and the numerous possibilities for structural diversification. In the last decade, they have been intensively studied as targets for potential anticancer therapeutics, producing a steady yearly rise in the number of published research articles. Many pyrazoline derivatives have shown remarkable cytotoxic activities in the form of heterocyclic or non-heterocyclic based hybrids, such as with coumarins, triazoles, and steroids. The enormous amount of related literature in the last 5 years prompted us to collect all these published data from screening against cancer cell lines, or protein targets like EGFR and structure activity relationship studies. Therefore, in the present review, a comprehensive account of the compounds containing the pyrazoline nucleus will be provided. The chemical groups and the structural modifications responsible for the activity will be highlighted. Moreover, emphasis will be given on recent examples from the literature and on the work of research groups that have played a key role in the development of this field.

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Section: 2-pyrazolinesmentioning

confidence: 99%

Pyrazoline Hybrids as Promising Anticancer Agents: An Up-to-Date Overview

Matiadis

Sagnou

2020

IJMS

104

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“…For antimalarial activity, the pyrazoline derivatives were tested against chloroquine-sensitive and chloroquine-resistant P. falciparum strains [44]. The new compounds were screened for in vitro, antimicrobial activity against some pathogenic microbial strains [46]. The bischalcones and bispyrazolines structures were confirmed by 1 H NMR, 13 C NMR, IR and Mass spectroscopy.…”

Section: Antimicrobial Activity Of Pyrazoline Derivativesmentioning

confidence: 99%

A Review on Pyrazoline Derivatives as Antimicrobial Agent

Jain

Singhal

2020

Int J Pharm Pharm Sci

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At present, there is a lot of research about the pyrazoline heterocyclic compound, its ring structure is being changed and new derivatives are being made, many of which have antimicrobial activity over the derivatives. Pyrazoline is the five-member heterocyclic ring which have two N atoms in nearby position and contains two endocyclic double bonds. Noteworthy consideration has been concentrated on pyrazolines and pyrazoline derivative due to their important pharmacological action. Some replaced pyrazolines have been stated near retain particular important pharmacological actions as antimicrobial, antifungal, antineoplastic, antidepressant, insecticidal, anticonvulsant, anti-inflammatory, antibacterial and antitumor properties.

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“…46,47 On the other hand, Zhao et al concluded that the 4,5-dihydropyrazole derivatives bearing thiazole and thiophene moieties IIa-c produced effective antiproliferative activity against WM266.4 and MCF-7 cell lines through BRAF V600E inhibitory activity. 48 While Sadashiva and coworkers have investigated the dual anticancer activity against A549 and MCF-7 human cancer cell lines as well as antimicrobial activity of the derivatives bearing thiazole heterocycle linked with pyrazoline moiety via carbohydrazide linker as compounds IIIa-c. 49 Furthermore, the thiazolinepyrazolines IV-VI represented promising cytotoxic effects and different RTKs suppressing impact while, the thiazolopyrazolyl coumarin derivatives VIIa, b exhibited signicant in vitro anticancer potentiality against different human cancer cell lines via a remarkable inhibition of VEGFR-2 with no noticeable toxicity towards the normal cells HFB4. 50 In addition, Vaarla et al have designed and synthesized the thiazolyl-3-arylpyrazole-4carbaldehydes VIIIa, b as signicant antimicrobial and cytotoxic agents against HeLa cell line and the docking simulation study validated different types of interactions with human microsomal cytochrome P450 (1z11.pdb) enzyme 51 (Fig.…”

Section: Introductionmentioning

confidence: 99%