Biological Evaluation of Isoniazid Derivatives as an Anticancer Class

Rodrigues, Felipe Augusto Rocha; Oliveira, Augusto César Aragão; Cavalcanti, Bruno C.; Pessoa, Cláudia; Pinheiro, Alessandra C.; Souza, Marcus V. N. de

doi:10.3797/scipharm.1307-25

Cited by 42 publications

(28 citation statements)

References 12 publications

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“…Then, compounds 5–11 reacted with benzhydrazide derivatives (3-chlorobenzhydrazide and 2,4-dichlorobenzhydrazide), and thiosemicarbazide or 4-substituted-3-thiosemicarbazide derivatives (4-phenyl-3-thiosemicarbazide and 4-(4-methylphenyl)-3-thiosemicarbazide) in the presence of anhydrous ethanol. The result of this reaction was obtaining target compounds: hydrazones 12–21 and thiosemicarbazones 22–28 . The synthesis of these compounds 12–28 was achieved through an efficient synthetic route outlined in Figure 2 .…”

Section: Resultsmentioning

confidence: 99%

Synthesis and in vitro antiproliferative and antibacterial activity of new thiazolidine-2,4-dione derivatives

Trotsko

Przekora

Zalewska

et al. 2017

Journal of Enzyme Inhibition and Medicinal Chemistry

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In our present research, we synthesised new thiazolidine-2,4-diones (12–28). All the newly synthesised compounds were evaluated for antiproliferative and antibacterial activity. Antiproliferative evaluation was carried out using normal human skin fibroblasts and tumour cell lines: A549, HepG2, and MCF-7. The IC50 values were determined for tested compounds revealing antiproliferative activity. Moreover, safety index (SI) was calculated. Among all tested derivatives, the compound 18 revealed the highest antiproliferative activity against human lung, breast, and liver cancer cells. More importantly, the derivative 18 showed meaningfully lower IC50 values when compared to the reference substance, irinotecan, and relatively high SI values. Moreover, newly synthesised compounds were screened for the bacteria growth inhibition in vitro. According to our screening results, most active compound was the derivative 18 against Gram-positive bacteria. Therefore, it may be implied that the novel compound 18 appears to be a very promising agent for anticancer treatment.

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Section: Resultsmentioning

confidence: 99%

Synthesis and in vitro antiproliferative and antibacterial activity of new thiazolidine-2,4-dione derivatives

Trotsko

Przekora

Zalewska

et al. 2017

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…Hydrazide is an organic compound with a core hydrazine functional group and at least one hydrogen atom replaced by a substituent containing an acyl group. There is increasing interest among researchers in the development of hydrazide compounds, as they have been demonstrated to have a range of activities including antituberculosis [1], anticancer [2], analgesic, anti-inflammatory [3], anti-human immunodeficiency virus (HIV) [4], antidiabetic [5] and antimalarial [6] effects.…”

Section: Introductionmentioning

confidence: 99%

Bis(N′-(3-chlorobenzoyl)isonicotinohydrazide)iron(III) Complex

Mardianingrum

Susanti

Ruswanto

2019

Molbank

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The bis(N′-(3-chlorobenzoyl)isonicotinohydrazide)iron(III) complex was synthesised from N′-(3-chlorobenzoyl)isonicotinohydrazide and iron(III) metal by reflux in an ethanol solution. The title compound was characterised by Fourier-transform infrared spectroscopy (FTIR) spectroscopy, differential thermal analysis/thermogravimetric analysis (DTA/TGA) and UV-visible spectroscopy. The results indicate that coordination of the iron(III) ion to the ligand increased its thermal stability.

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“…In-vitro anti tubercular activity [13] The anti-mycobacterial activity of Unsaponifiable matter of Serankottai nei was assessed against Mycobacterium tuberculosis (H37Rv strain from ATCC, No-27294) using microplate Alamar Blue assay (MABA). This methodology is nontoxic, uses a thermally stable reagent and shows good correlation with proportional and BACTEC radiometric method.…”

Section: Test For Quininementioning

confidence: 99%

Phytochemical Standardization of Serankottai nei (a Siddha drug from milk extract of Semecarpus Anacardium nuts) and its in-vitro antitubercular activity against H37Rv strain

Senthilvel¹,

Amuthan²,

Kumar³

2016

IJPCS

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Background: Serankottai nei is a popular Siddha drug, used in the treatment of lung infections including tuberculosis, autoimmune joint diseases (rheumatoid arthritis, degenerative osteoarthritis), cancers and neurological pain. Objective: To standardize serankottai nei and to screen its in-vitro antitubercular activity of in H37Rv strain. Materials and Methods: Serankottai nei, a medicated ghee preparation was procured from the SKM Siddha and Ayurveda Co India Ltd, Erode, Tamil Nadu. Unsaponifiable matter (USM) from the ghee preparation was separated and preliminary phytochemical screening was done. Further, USM was dissolved in 10 ml of chloroform and 3 and 6 µl of the above sample was applied for HPTLC fingerprint, which was developed in toluene: ethyl acetate (9.0:1.0). The developed plates were scanned under UV 254 nm, 366 nm, 540 nm and 620 nm post derivatization. R f , colour of the spots and densitometric scan were recorded. Different doses of USM were screened for in-vitro antitubercular activity against H37Rv strain using Alamar Blue Dye method. Results: Phytochemical screening of 8% w/w USM obtained from serankottai nei showed presence of alkaloid, phenol, steroid and terpenoid. In HPTLC, there were 15, 5 and 7 peaks at 254 nm, 366 nm and 620 nm respectively. The Minimum Inhibitory Concentration (MIC) against H37Rv strain of pyrazinamide, streptomycin, ciprofloxacin were 3.125, 6.25 and 3.125 µg/ml respectively. Whereas, the MIC of serankottai nei was 1.6 µg/ml, which was almost 25 to 50% of standard drugs. Conclusion: Serankottai nei has shown promising antitubercular activity in in-vitro study. Thus, Semecarpus anacardium could be a suitable candidate for a new herbal based antitubercular drug.

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Biological Evaluation of Isoniazid Derivatives as an Anticancer Class

Cited by 42 publications

References 12 publications

Synthesis and in vitro antiproliferative and antibacterial activity of new thiazolidine-2,4-dione derivatives

Synthesis and in vitro antiproliferative and antibacterial activity of new thiazolidine-2,4-dione derivatives

Bis(N′-(3-chlorobenzoyl)isonicotinohydrazide)iron(III) Complex

Phytochemical Standardization of Serankottai nei (a Siddha drug from milk extract of Semecarpus Anacardium nuts) and its in-vitro antitubercular activity against H37Rv strain

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