New Adamantyl Chalcones: Synthesis, Antimicrobial and Anticancer Activities

Tabbi, Aouatef; Tebbani, Dahmane; Caporale, Angelamaria; Saturnino, Carmela; Nabavi, Seyed Mohammad; Palma, Giuseppe; Arra, Claudio; Cantürk, Zerrin; Turan-Zitouni, Gülhan; Mérazig, Hocine; Sobarzo‐Sánchez, Eduardo; Rastrelli, Luca

doi:10.2174/1568026616666160824121935

Cited by 9 publications

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“…In addition to the aforementioned chalcone hybrids, other hybrids, such as chalcone–ferrocene [ 95 , 96 , 97 ], chalcone–furan/thiophene hybrids [ 98 , 99 , 100 , 101 ], chalcone–pyridine/pyrimidine hybrids [ 102 , 103 , 104 , 105 , 106 ], chalcone–quinoline/quinolone hybrids [ 107 , 108 , 109 , 110 , 111 ], chalcone–quinoxaline/quinazolinone hybrids [ 112 , 113 , 114 ], chalcone-quinone hybrids [ 115 , 116 , 117 ], chalcone–triazine hybrids [ 118 , 119 ], and chalcone–dithiocarbamate hybrids [ 120 , 121 ] also showed certain anticancer activity.…”

Section: Strategies Employed To Produce Anticancer Chalconesmentioning

confidence: 99%

Chalcone Derivatives: Role in Anticancer Therapy

et al. 2021

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Chalcones (1,3-diaryl-2-propen-1-ones) are precursors for flavonoids and isoflavonoids, which are common simple chemical scaffolds found in many naturally occurring compounds. Many chalcone derivatives were also prepared due to their convenient synthesis. Chalcones as weandhetic analogues have attracted much interest due to their broad biological activities with clinical potentials against various diseases, particularly for antitumor activity. The chalcone family has demonstrated potential in vitro and in vivo activity against cancers via multiple mechanisms, including cell cycle disruption, autophagy regulation, apoptosis induction, and immunomodulatory and inflammatory mediators. It represents a promising strategy to develop chalcones as novel anticancer agents. In addition, the combination of chalcones and other therapies is expected to be an effective way to improve anticancer therapeutic efficacy. However, despite the encouraging results for their response to cancers observed in clinical studies, a full description of toxicity is required for their clinical use as safe drugs for the treatment of cancer. In this review, we will summarize the recent advances of the chalcone family as potential anticancer agents and the mechanisms of action. Besides, future applications and scope of the chalcone family toward the treatment and prevention of cancer are brought out.

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Section: Strategies Employed To Produce Anticancer Chalconesmentioning

confidence: 99%

Chalcone Derivatives: Role in Anticancer Therapy

et al. 2021

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“…Thiosemicarbazone derivatives, which play an important role in organic and medicinal chemistry, have attracted a large number of researchers over the years because of their promising biological activities, such as antioxidant [21,23], antiparasitic [10,14,34,37], anticonvulsant [16], antiviral [7,19,26],. Especially, in recent years, large of publications focused on synthesis and antimicrobial [5,15,27,28,35], anticancer [5,13,18,25,28,32,41] activity of thiosemicarbazones to find out the potential candidates to develop new drugs.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Bioactivity of Thiosemicarbazones Containing Adamantane Skeletons

Pham¹,

Phan²,

Phan³

et al. 2021

Prime Archives in Molecular Sciences

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Reaction of 4-(1-adamantyl)-3-thiosemicarbazide (1) with numerous substituted acetophenones and benzaldehydes yielded the corresponding thiosemicarbazones containing adamantane skeletons. The synthesized compounds were evaluated for their in vitro activities against some Gram-positive and Gramnegative bacteria, and the fungus Candida albicans, and cytotoxicity against four cancer cell lines (Hep3B, HeLa, A549, and MCF-7). All of them showed good antifungal activity against Candida albicans. Compounds 2c, 2d, 2g, 2j and 3a, 3e, 3g displayed significant inhibitory activity against Enterococcus faecalis. Compounds 2a, 2e, 2h, 2k and 3j had moderate inhibitory potency against Staphylococcus aureus. Compounds 2a, 2e and 2g found so good inhibitory effect on Bacillus cereus. Compounds 2d and 2h, which contain (ortho) hydroxyl groups on the phenyl ring, were shown to be good candidates as potential agents for killing the tested cancer cell lines, i.e., Hep3B, A549, and MCF-7. Compounds 2a-c, 2f, 2g, 2j, 2k, 3g, and 3i were moderate inhibitors against MCF-7.

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“…A number of studies were conducted, focusing on such derivatives with the hope to find new compounds and biological activities. As a result, many adamantane derivatives were discovered with numerous biological activities, such as antiviral [15][16][17][18][19][20], antimicrobial [18,[20][21][22][23][24][25][26][27][28][29][30], anticancer [23,27,[31][32][33][34][35], angiogenesis inhibition [36], anti-inflammation [37], 11β hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibition [38][39][40], and tyrosinase inhibition [41] activities. Among them, nine compounds were approved for use in clinics, including amantadine, memantine, rimantadine, tromantadine, adapalene, vildagliptine, saxagliptine, bromanatane, and adapromine.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Bioactivity of Hydrazide-Hydrazones with the 1-Adamantyl-Carbonyl Moiety

Pham¹,

Phan²,

Phan³

et al. 2021

Prime Archives in Molecular Sciences

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Reaction of 1-adamantyl carbohydrazide (1) with various substituted benzaldehydes and acetophenones yielded the corresponding hydrazide-hydrazones with a 1-adamantane carbonyl moiety. The new synthesized compounds were tested for activities against some Gram-negative and Gram-positive bacteria, and the fungus Candida albicans. Compounds 4a, 4b, 5a, and 5c displayed potential antibacterial activity against tested Gram-positive bacteria and C. albicans, while compounds 4e and 5e possessed cytotoxicity against tested human cancer cell lines.

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New Adamantyl Chalcones: Synthesis, Antimicrobial and Anticancer Activities

Abstract: The effect of these compounds was also tested in vitro as antitumor on Miapaca2 cells. Compounds also showed anticancer activity against human pancreas cancer cell MiaPaca2.

Cited by 9 publications

References 0 publications

Chalcone Derivatives: Role in Anticancer Therapy

Chalcone Derivatives: Role in Anticancer Therapy

Synthesis and Bioactivity of Thiosemicarbazones Containing Adamantane Skeletons

Synthesis and Bioactivity of Hydrazide-Hydrazones with the 1-Adamantyl-Carbonyl Moiety

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