Synthesis and Preliminary Antimicrobial Analysis of Isatin–Ferrocene and Isatin–Ferrocenyl Chalcone Conjugates

Singh, Amandeep; Fong, Grant; Liu, Jenny; Wu, Ying-Hsin; Chang, Kevin Chen-Chuan; Park, William; Kim, Ji‐Hwan; Tam, Christina; Cheng, Luisa W.; Land, Kirkwood M.; Kumar, Vipan

doi:10.1021/acsomega.8b00553

Cited by 30 publications

(18 citation statements)

References 51 publications

(69 reference statements)

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“…In another study, a series (132–179) of isatin–ferrocenyl chalcone and isatin–ferrocene conjugates were synthesized and were evaluated for their inhibitory activities against T. vaginalis. The compounds exhibited 100% growth inhibition ( Singh et al, 2018 ). In another study, three chalcones, diuvaretin, uvaretin, and isouvaretin, were investigated on their antibacterial activity, and the culture inhibition was only observed for Gram-positive germs ( Koudokpon et al, 2018 ).…”

Section: Preclinical Pharmacological Activities Of Chalconesmentioning

confidence: 99%

Pharmacological Properties of Chalcones: A Review of Preclinical Including Molecular Mechanisms and Clinical Evidence

et al. 2021

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Chalcones are among the leading bioactive flavonoids with a therapeutic potential implicated to an array of bioactivities investigated by a series of preclinical and clinical studies. In this article, different scientific databases were searched to retrieve studies depicting the biological activities of chalcones and their derivatives. This review comprehensively describes preclinical studies on chalcones and their derivatives describing their immense significance as antidiabetic, anticancer, anti-inflammatory, antimicrobial, antioxidant, antiparasitic, psychoactive, and neuroprotective agents. Besides, clinical trials revealed their use in the treatment of chronic venous insufficiency, skin conditions, and cancer. Bioavailability studies on chalcones and derivatives indicate possible hindrance and improvement in relation to its nutraceutical and pharmaceutical applications. Multifaceted and complex underlying mechanisms of chalcone actions demonstrated their ability to modulate a number of cancer cell lines, to inhibit a number of pathological microorganisms and parasites, and to control a number of signaling molecules and cascades related to disease modification. Clinical studies on chalcones revealed general absence of adverse effects besides reducing the clinical signs and symptoms with decent bioavailability. Further studies are needed to elucidate their structure activity, toxicity concerns, cellular basis of mode of action, and interactions with other molecules.

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Section: Preclinical Pharmacological Activities Of Chalconesmentioning

confidence: 99%

Pharmacological Properties of Chalcones: A Review of Preclinical Including Molecular Mechanisms and Clinical Evidence

et al. 2021

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“…Furthermore, heterocyclic chalcones ( 173, 175, 176, 181 , and 184 ) showed lower to larger IC 50 values, and chalcones with extended hetero functionality ( 177, 178, 179, 182, 183, and 186 ) were found to be the best in the broad-spectrum cancer cell lines, as indicated in the table. Moreover, chalcones with nitrogen- and sulfur-containing heterocycles and with methoxy substitutions have been reported to be active against microbes, leukemia, prostate cancer, and colon cancer [ 218 , 219 , 220 , 221 , 222 , 223 , 224 , 225 , 226 , 227 , 228 , 229 , 230 , 231 , 232 , 233 , 234 , 235 ].…”

Section: Chalcones For Non-infectious Diseasesmentioning

confidence: 99%

Chalcone: A Promising Bioactive Scaffold in Medicinal Chemistry

et al. 2022

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Chalcones are a class of privileged scaffolds with high medicinal significance due to the presence of an α,β-unsaturated ketone functionality. Numerous functional modifications of chalcones have been reported, along with their pharmacological behavior. The present review aims to summarize the structures from natural sources, synthesis methods, biological characteristics against infectious and non-infectious diseases, and uses of chalcones over the past decade, and their structure–activity relationship studies are detailed in depth. This critical review provides guidelines for the future design and synthesis of various chalcones. In addition, this could be highly supportive for medicinal chemists to develop more promising candidates for various infectious and non-infectious diseases.

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“…Isatin is a heterocyclic scaffold that is isolated from the leaves and roots of Couroupita guianesis and Calanthe discolour, Isatis tinctoria and it is found to be versatile in organic synthesis because of the many possibilities of modification at C-3, C-5, and N-1 with various activities such as anticancer, antimalarial, and antifungal [46,47,48]. Kumar et al synthesized several isatin–ferrocene conjugates tethered with 1 H -1,2,3-triazole derivatives ( 32a – h ) via copper-promoted azide–alkyne cycloaddition reaction and tested them against chloroquine-resistant strains (3D7 and W2) of P. falciparum (Figure 13) [47].…”

Section: Ferrocene-based Compounds With Antimalaria Activitymentioning

confidence: 99%

Ferrocene-Based Compounds with Antimalaria/Anticancer Activity

2019

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Malaria and cancer are chronic diseases. The challenge with drugs available for the treatment of these diseases is drug toxicity and resistance. Ferrocene is a potent organometallic which have been hybridized with other compounds resulting in compounds with enhanced biological activity such as antimalarial and anticancer. Drugs such as ferroquine were developed from ferrocene and chloroquine. It was tested in the 1990s as an antimalarial and is still an effective antimalarial. Many researchers have reported ferrocene compounds as potent compounds useful as anticancer and antimalarial agents when hybridized with other pharmaceutical scaffolds. This review will be focused on compounds with ferrocene moieties that exhibit either an anticancer or antimalarial activity.

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Synthesis and Preliminary Antimicrobial Analysis of Isatin–Ferrocene and Isatin–Ferrocenyl Chalcone Conjugates

Cited by 30 publications

References 51 publications

Pharmacological Properties of Chalcones: A Review of Preclinical Including Molecular Mechanisms and Clinical Evidence

Pharmacological Properties of Chalcones: A Review of Preclinical Including Molecular Mechanisms and Clinical Evidence

Chalcone: A Promising Bioactive Scaffold in Medicinal Chemistry

Ferrocene-Based Compounds with Antimalaria/Anticancer Activity

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