One-pot multicomponent synthesis of novel thiazolylhydrazone derivatives and their antimicrobial activity

Rajitha, Galla; Velpula, Ravibabu; Ramesh, Gali; Rajitha, B.; Rajkumari, Jobina; Siddhardha, Busi; Laxmi, S. Vijaya

doi:10.1007/s11164-015-1959-8

Cited by 12 publications

(9 citation statements)

References 28 publications

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“…The methods used in the biological studies (antibacterial, antifungal, antioxidant and in vitro antiproliferative activity studies) were done according to reported procedures …”

Section: Methodsmentioning

confidence: 99%

Unusual coordination mode of aroyl/acyl thiourea ligands and their π‐arene ruthenium (II) piano‐stool complexes: Synthesis, molecular geometry, theoretical studies and biological applications

Rohini

Konakanchi

Prashanth

et al. 2019

Applied Organom Chemis

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Two mononuclear ruthenium complexes (1 and 2) with aroyl/acylthiourea as an ancillary ligand of type, [(η6‐p‐cymene)RuCl(L‐N,S)], where [L1 = 2,4‐dichloro‐N‐(o‐tolylcarbamothioyl)benzamide] and L2 = N‐(phenylcarbamothioyl)cyclohexanecarboxamide] were synthesized and well characterized. The single crystal X‐ray diffraction studies revealed the coordination mode and the geometry of the complexes. The two complexes adopted general piano‐stool (three‐legged) geometry with a novel coordination mode of aroyl/acylthiourea through amide N (anionic) and thiocarbonyl S (neutral). This type of monobasic bidentate coordination of the aroyl/acylthiourea ligand was witnessed the first time around the metal ion. The coordination of the complexes was well explained through geometric parameters and frontier molecular orbital parameter values computed at the B3LYP/SDD level. The synthesized complexes were also screened for their antibacterial, antifungal, antioxidant and in vitro antiproliferative activities. Complexes exhibited good antimicrobial agents against various pathogens. The antioxidant activity of the complex 2 has shown most potent activity with IC50 value of 48.55 ± 1.7 μM compared to the reference drug. In addition, the in vitro antiproliferative activity of the complex 2 showed excellent activity against HepG‐2 cell line with the IC50 value of 24.30 ± 1.20 μM which is close to Doxorubicin standard drug.

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“…The methods used in the biological studies (antibacterial, antifungal, antioxidant and in vitro antiproliferative activity studies) were done according to reported procedures …”

Section: Methodsmentioning

confidence: 99%

Unusual coordination mode of aroyl/acyl thiourea ligands and their π‐arene ruthenium (II) piano‐stool complexes: Synthesis, molecular geometry, theoretical studies and biological applications

Rohini

Konakanchi

Prashanth

et al. 2019

Applied Organom Chemis

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“…In continuation of our interest regarding synthesis of various biologically active novel heterocycles [37,38], we designed synthesis of novel 1-thiazolyl-5-coumarin-3-ylpyrazole derivatives. To analyze the synthetic route, the model reaction was carried out for the synthesis of product 4a by using salicylaldehyde (1a), 4-hydroxy-6-methyl-2H-pyran-2-one (2) and 2-hydrazinyl-4-arylthiazoles (3a) in acetonitrile with a catalytic amount of piperidine under reflux conditions.…”

Section: Resultsmentioning

confidence: 99%

One-pot multicomponent synthesis of novel 1-thiazolyl-5-coumarin-3-yl-pyrazole derivatives and evaluation of their cytotoxic activity

et al. 2015

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A series of novel 1-thiazolyl-5-coumarin-3-yl-pyrazole derivatives (4a-l) were synthesized via one-pot multicomponent reaction of 5-substituted salicylaldehydes (1a-c), 4-hydroxy-6-methyl-2H-pyran-2-one (2) and 2-hydrazinyl-4-arylthiazoles (3a-d) in acetonitrile using a catalytic amount of piperidine under reflux conditions. This multicomponent approach has advantages such as reduced reaction time and a high product yield percentage when compared with corresponding multistep approaches. All the synthesized compounds were evaluated for their cytotoxic activity against Hep G2 (hepatocellular liver carcinoma) and MCF-7 (breast cancer) cell lines and compared with the standard drug Doxorubicin. Among all the compounds, compounds 4d against Hep G2, 4k against MCF-7 and 4e against both Hep G2 & MCF-7 showed excellent cytotoxic activity.

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“…Cancer is a chief reason of health disquiet with a startling growth in several patients all over the world . As per data; cancer is the second most disease that effect on human transience after the cardiac disease.…”

Section: Figurementioning

confidence: 99%

Design and Synthesis of Some Novel Aromatic Amide Derivatives of Nilutamide as In Vitro Anticancer Agents

Thirukovela¹,

Nukala²,

Narsimha³

et al. 2020

ChemistrySelect

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The synthesis of some new aromatic amide derivatives of Nilutamide (4 an) and their structure determination using 1 H NMR, 13 C NMR and mass spectral analysis was described. The in vitro anti-cancer activity of the compounds (4 an) against several human cancer cell lines like PC3 (prostate), A549 (lung), MCF-7 (breast) and DU-145 (prostate) revealed that the compounds 4 c, 4 h, 4 l, 4 m and 4 n have shown greater activity against all the cell lines than the standard Etoposide. Predominantly, the compound 4 n was displayed excellent activity over PC3, A549, MCF-7 and DU-145 with IC 50 values of 0.14, 0.10, 0.19 and 0.63 μM respectively. Moreover, molecular docking studies of derivatives (4 an) on EGFR receptor suggested that the most potent compound 4 n strongly binds to protein EGFR (pdb id : 4HJO). The energy calculations of in silico studies were also in good agreement with the obtained IC 50 values.

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One-pot multicomponent synthesis of novel thiazolylhydrazone derivatives and their antimicrobial activity

Cited by 12 publications

References 28 publications

Unusual coordination mode of aroyl/acyl thiourea ligands and their π‐arene ruthenium (II) piano‐stool complexes: Synthesis, molecular geometry, theoretical studies and biological applications

Unusual coordination mode of aroyl/acyl thiourea ligands and their π‐arene ruthenium (II) piano‐stool complexes: Synthesis, molecular geometry, theoretical studies and biological applications

One-pot multicomponent synthesis of novel 1-thiazolyl-5-coumarin-3-yl-pyrazole derivatives and evaluation of their cytotoxic activity

Design and Synthesis of Some Novel Aromatic Amide Derivatives of Nilutamide as In Vitro Anticancer Agents

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