Novobiocin–ferrocene conjugates possessing anticancer and antiplasmodial activity independent of HSP90 inhibition

Mbaba, Mziyanda; Mare, Jo‐Anne de la; Sterrenberg, Jason N.; Kajewole, Deborah; Maharaj, Shantal; Edkins, Adrienne L.; Isaacs, Michelle; Hoppe, Heinrich C.; Khanye, Setshaba D.

doi:10.1007/s00775-018-1634-9

Cited by 26 publications

(28 citation statements)

References 44 publications

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“…It was reported that these three compounds were selective towards the P. falciparum parasite and their HeLa cell viability was below 25% with no toxic effects [44]. Novobiocin and other derivatives from this series of compounds were inactive with HeLa cell viability that was greater than 75%, which means N-methyl substituents play an important role in the antiplasmodial activity of these compounds and also these compounds were found to be independent of Hsp90 [44].…”

Section: Ferrocene-based Compounds With Antimalaria Activitymentioning

confidence: 97%

“…Novobiocin is an antibiotic that is produced by bacteria called Streptomyces, its inhibitor of the chaperone, heat shock protein 90 (Hsp90) which is responsible for the stabilization of proteins and it is found to be one of the antibiotics that are biological active with anticancer and antimalarial activity when it is incorporated together with other active molecules such as ferrocene [42,43,44].…”

Section: Ferrocene-based Compounds With Antimalaria Activitymentioning

confidence: 99%

“…Mbaba et al reported another series of ferrocene–novobiocin derivatives and evaluated them for antiplasmodial activity and human cytotoxicity using the 3D7 strain of P. falciparum and HeLa cells, respectively, in vitro. Compound 29a – c which contain the N -methyl group in the piperidine ring exhibited better antimalarial activity with IC 50 values that were below 10 μM but compound 29c was the most potent compound with an IC 50 value of 0.889 μM [44]. It was reported that these three compounds were selective towards the P. falciparum parasite and their HeLa cell viability was below 25% with no toxic effects [44].…”

Section: Ferrocene-based Compounds With Antimalaria Activitymentioning

confidence: 99%

“…Compound 29a – c which contain the N -methyl group in the piperidine ring exhibited better antimalarial activity with IC 50 values that were below 10 μM but compound 29c was the most potent compound with an IC 50 value of 0.889 μM [44]. It was reported that these three compounds were selective towards the P. falciparum parasite and their HeLa cell viability was below 25% with no toxic effects [44]. Novobiocin and other derivatives from this series of compounds were inactive with HeLa cell viability that was greater than 75%, which means N-methyl substituents play an important role in the antiplasmodial activity of these compounds and also these compounds were found to be independent of Hsp90 [44].…”

Section: Ferrocene-based Compounds With Antimalaria Activitymentioning

confidence: 99%

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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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Section: Ferrocene-based Compounds With Antimalaria Activitymentioning

confidence: 97%

Section: Ferrocene-based Compounds With Antimalaria Activitymentioning

confidence: 99%

Section: Ferrocene-based Compounds With Antimalaria Activitymentioning

confidence: 99%

Section: Ferrocene-based Compounds With Antimalaria Activitymentioning

confidence: 99%

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Ferrocene-Based Compounds with Antimalaria/Anticancer Activity

2019

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“…Besides the abovementioned coumarin hybrids, coumarin–pyridine hybrids, [ 116–118 ] coumarin–imine hybrids, [ 119–122 ] coumarin–peptide hybrids, [ 123 ] coumarin–indole hybrids, [ 124 ] coumarin–sulfonamide hybrids, [ 125 ] coumarin–ferrocene hybrids, [ 126 ] coumarin–thiazine hybrids, [ 127 ] coumarin–sugar hybrids, [ 128 ] coumarin–pyran hybrids, [ 129 ] and coumarin–glyoxal hybrids [ 130 ] also showed certain antibacterial activity, but the majority of them were far less potent than the reference drugs. Hence, the enriched SAR may pave the way for further rational design of the novel coumarin hybrids.…”

Section: Miscellaneous Coumarin Hybridsmentioning

confidence: 99%

Coumarin‐containing hybrids and their antibacterial activities

Feng

Zhang

Yang

et al. 2020

Archiv der Pharmazie

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Infections caused by Gram-positive and -negative bacteria are one of the foremost causes of morbidity and mortality globally. Antibiotics are the mainstay of therapy for bacterial infections, but the emergence and wide spread of drug-resistant pathogens have already become a huge issue for public healthcare systems. The coumarin moiety, which is ubiquitous in nature, could bind to the B subunit of DNA gyrase in bacteria and inhibit DNA supercoiling by blocking the ATPase activity; hence, coumarin derivatives possess potential antibacterial activity. Several coumarin-containing hybrids such as coumermycin A1, clorobiocin, and novobiocin have already been used in clinical practice for the treatment of various bacterial infections; thus, it is conceivable that hybridization of the coumarin moiety with other antibacterial pharmacophores may provide opportunities for the development of novel antibiotics. This review outlines the advances in coumarin-containing hybrids with antibacterial potential in the recent 5 years and the structure-activity relationships are also discussed. K E Y W O R D S antibacterial, coumarin, hybrid compounds, structure-activity relationships

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Coumarin derivatives with anticancer activities: An update

Song

Fan

Liu

et al. 2020

Archiv der Pharmazie

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Cancer can invade or spread to almost all parts of the body. The increasing morbidity and high mortality of cancer create a great demand for the development of novel anticancer drugs. Coumarin derivatives are ubiquitous in nature and can readily interact with diverse enzymes and receptors in cancer cells via weak bond interactions; hence, coumarin is a highly privileged pharmacophore for the development of novel anticancer agents. This review will focus on the recent development of coumarin hybrids as potential anticancer agents covering articles published from 2019 to 2020.

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Novobiocin–ferrocene conjugates possessing anticancer and antiplasmodial activity independent of HSP90 inhibition

Cited by 26 publications

References 44 publications

Ferrocene-Based Compounds with Antimalaria/Anticancer Activity

Ferrocene-Based Compounds with Antimalaria/Anticancer Activity

Coumarin‐containing hybrids and their antibacterial activities

Coumarin derivatives with anticancer activities: An update

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