Chloro and bromo-pyrazole curcumin Knoevenagel condensates augmented anticancer activity against human cervical cancer cells: design, synthesis, <i>in silico</i> docking and <i>in vitro</i> cytotoxicity analysis

Chaudhary, Monika; Kumar, Neeraj; Baldi, Ashish; Chandra, Ramesh; Babu, M. Arockia; Madan, Jitender

doi:10.1080/07391102.2019.1578264

Cited by 38 publications

(16 citation statements)

References 41 publications

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“…Addition of bromine to the furan‐chalcone 6c resulted in an efficient larvicidal compound with respect to its concentration, length of action and toxicity profile to other organisms. This substituent also effectively enhances the biological activity of other molecules 91–94 . Compared with compound 6d , compound 6c presented lower LC 50 and LC 90 values to kill Ae.…”

Section: Discussionmentioning

confidence: 96%

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Larvicidal activity of substituted chalcones against Aedes aegypti (Diptera: Culicidae) and non‐target organisms

Targanski

Sousa

Pádua

et al. 2020

Pest Management Science

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BACKGROUND: The expansion of Aedes aegypti (Diptera: Culicidae) population has increased the number of cases of arboviruses, in part due to the inefficiency and toxicity of the chemical control methods available to control this vector. We synthesized 19 chalcone derivatives and examined their activity against Ae. aegypti larvae in order to select larvicidal compounds that are non-toxic to other organisms. RESULTS: Seven chalcone derivatives (3a, 3e, 3f, 6a, 6c, 6d, and 6f) had lethal concentrations of substituted chalcones capable of killing 50% (LC 50) values lower than 100 mg mL −1 at 24 h post-treatment, which is the dose that the World Health Organization recommends for the selection of promising larvicides. The type of substituent added to (E)-1,3-diphenylprop-2-en-1-one (3a) markedly affected the larvicidal activity. Addition of chlorine, bromine and methoxy groups to the aromatic rings reduced the larvicidal activity, while replacement of the Bring (phenyl) by a furan ring significantly increased the larvicidal activity. The furan-chalcone (E)-3-(4-bromophenyl)-1-(furan-2-yl)prop-2-en-1-one (6c) killed Ae. aegypti larvae (LC 50 = 6.66 mg mL −1 ; LC 90 = 9.97 mg mL −1) more effectively than the non-substituted chalcone (3a) (LC 50 = 14.43 mg mL −1 ; LC 90 = 20.96 mg mL −1), and was not toxic to the insect Galleria mellonella, to the protozoan Tetrahymena pyriformis, and to the algae Chorella vulgaris. CONCLUSIONS: The substitution pattern of chalcones influenced their larvicidal activity. In the set of compounds tested, (E)-3-(4-bromophenyl)-1-(furan-2-yl)prop-2-en-1-one (6c) was the most effective larvicide against Ae. aegypti, with no clear signs of toxicity to other animal models. Its mechanism of action and effectiveness under field conditions remain to be determined.

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Section: Discussionmentioning

confidence: 96%

“…This substituent also effectively enhances the biological activity of other molecules. [91][92][93][94] Compared with compound 6d, compound 6c presented lower LC 50 and LC 90 values to kill Ae. aegypti (L3) larvae and had the advantage of not interfering with the growth of the four environmental indicator organisms.…”

Section: Discussionmentioning

confidence: 97%

Larvicidal activity of substituted chalcones against Aedes aegypti (Diptera: Culicidae) and non‐target organisms

Targanski

Sousa

Pádua

et al. 2020

Pest Management Science

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“…Percentage of curcumin range from 2.85 to 6.5 %. [19,24,29,[33][34][35][36] Solvent for extraction using Soxhlet apparatus: Ethanol…”

Section: Major Active Constituent Api[28]mentioning

confidence: 99%

A Comparative Review on the Standard Quality Parameters of Turmeric

Singh¹,

Bajwa²,

Baldi³

2021

IJNP

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The world economy of the international trade of herbs and related products has been witnessing an increase of 15% annually. In the aftermath of the COVID-19 outbreak, there are reports highlighting an instant rise in the demand for medicinal plants especially the immunity booster plants. Due to the anti-oxidant, anti-inflammatory, anti-viral, anti-bacterial and antifungal properties of Curcuma longa L. popularly known as Turmeric and Haldi in India, herbal scientists are exploring this potential herb in managing the COVID-19 pandemic. It is widely believed that an increase in the demand for herbal products may increase the chances of species adulteration leading to adverse consequences. In such cases, it is important to devise a comprehensive intuitive document highlighting various standard quality parameters of Turmeric that are reported in different standard texts benefitting the concerned stakeholders. In the present review, classical texts such as API (Ayurvedic Pharmacopoeia of India), WHO (World Health Organization), FSSAI (Food Safety and Standards Authority of India) and other literature are explored to highlight standard quality parameters of Turmeric.

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“…In this way, the molecular docking, a computational strategy that allows one to predict binding site complementarity between a drug and its therapeutic target, has been massively used to assist drug repositioning for several diseases [6] , [9] . For example, in silico simulations were used to evaluate non-nucleoside reverse transcriptase inhibitors for HIV treatment [10] , as well as currently used drugs against HIV-1 protease of subtype D [11] ; to study the substrate recognition processes for influenza drug targets [12] , [13] ; to investigate and screening inhibitors against Ebola virus [14] , [15] , [16] ; to explore potential binding pockets and inhibitors for Zika [17] , [18] , Chikungunya [19] and Dengue virus [20] , [21] ; to perform structure-based virtual screening studies of potential drug target of Leishmania donovani [22] ; to evaluate the anticancer activity of chloro and bromo-pyrazole curcumin knoevenagel condensates and phytoestrogens [23] , [24] ; to investigate the efficacy of direct acting antivirals (DAAs) to the treatment of different Hepatitis C virus [25] and to design modified peptidomimetic cellulose derivatives Hepatitis C virus protease inhibitors [26] . In addition, in silico simulationshave have also been used to evaluate potential inhibitors of the interaction between ACE2 and SARS-CoV-2 region binding domain [27] , to help in the drug repositioning of anti-Hepatitis C virus drugs [28] and anti-polymerase drugs [29] against SARS-CoV-2.…”

Section: Introductionmentioning

confidence: 99%

Molecular dynamics simulation of docking structures of SARS-CoV-2 main protease and HIV protease inhibitors

Cardoso

Mendanha

2021

Journal of Molecular Structure

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Chloro and bromo-pyrazole curcumin Knoevenagel condensates augmented anticancer activity against human cervical cancer cells: design, synthesis, in silico docking and in vitro cytotoxicity analysis

Cited by 38 publications

References 41 publications

Larvicidal activity of substituted chalcones against Aedes aegypti (Diptera: Culicidae) and non‐target organisms

Larvicidal activity of substituted chalcones against Aedes aegypti (Diptera: Culicidae) and non‐target organisms

A Comparative Review on the Standard Quality Parameters of Turmeric

Molecular dynamics simulation of docking structures of SARS-CoV-2 main protease and HIV protease inhibitors

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