The authors aimed to estimate the therapeutic potential of novel chalcones against tuberculosis. 11 synthesized compounds were tested for antimycobacterial activity against (H37RV; American Type Culture Collection number: 27294) using the microplate alamarBlue assay. Molecular docking and pharmacokinetic parameter analyses were then performed. The most potent compounds, (2E)-1-(4-bromophenyl) (2E)-1-(2-nitrophenyl) prop-2-en-1-one, -3-(2-nitrophenyl) prop-2-en-1-one (4-bromophenyl) (2E)-1-(3-phenoxyphenyl)prop-2-en-1-one, 3-(phenoxyphenyl)prop-2-en-1-one (4-bromophenyl) prop-2-en-1-one and (2E)-1-(4-bromophenyl)-3-(5-chloro-2-hydroxyphenyl)-prop-2-en-1-one, showed activity, with a minimum inhibitory concentration (MIC) of 6.25 μg/ml. Compounds LSD2, LSD12, LSD13 and LSD15 showed strong antimycobacterial activity at a concentration of 6.25 μg/ml.
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http://dx.doi.org/10.4155/fmc-2022-0052 | DOI Listing |
Pharmaceuticals (Basel)
January 2025
School of Pharmacy and Pharmaceutical Sciences, Panoz Institute, Trinity College Dublin, D02 PN40 Dublin, Ireland.
The synthesis of ()-1-(1,3-diphenylallyl)-1-1,2,4-triazoles and related compounds as anti-mitotic agents with activity in breast cancer was investigated. These compounds were designed as hybrids of the microtubule-targeting chalcones, indanones, and the aromatase inhibitor letrozole. : A panel of 29 compounds was synthesized and examined by a preliminary screening in estrogen receptor (ER) and progesterone receptor (PR)-positive MCF-7 breast cancer cells together with cell cycle analysis and tubulin polymerization inhibition.
View Article and Find Full Text PDFInt J Mol Sci
January 2025
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
Cancer remains a leading cause of morbidity and mortality worldwide, highlighting the urgent need for novel therapeutic agents. This study investigated the synthesis and biological evaluation of -alkyl ()-chalcone derivatives (-) as potential anticancer agents. The compounds were synthesized via aldol condensation of substituted aldehydes and acetophenones, with structures confirmed by IR, NMR, and mass spectrometry.
View Article and Find Full Text PDFBioorg Chem
January 2025
Medicinal Chemistry Department, Faculty of Pharmacy, Suez Canal University, Ismailia 41522 Egypt. Electronic address:
Novel 1,2,3-triazole hybrids bearing various substituents have been synthesized as potential anticancer agents. Ligand-based approach has been adopted to design these compounds relying on the hybridization of 1,2,3-triazole with α,β-unsaturated carbonyl, 5- and 6-membered heterocyclic scaffolds. All synthesized members were investigated for their cytotoxic potency against nine types comprising 60 panels of human cancerous cells by the US National Cancer Institute: Development Therapeutic Program (US_NCI_DTP).
View Article and Find Full Text PDFBiochem Biophys Res Commun
January 2025
Molecular Biophysics and Structural Biology (MBSB) Group, Department of Biochemistry, University of Johannesburg, Auckland Park Kingsway Campus, 2006, South Africa. Electronic address:
To address microbial infections and combat drug resistance, we designed, synthesized, and evaluated three novel s-triazine clubbed pharmacophores: 1-acetylpyrazoline (5a-e), 2-aminopyrimidine (6a-e), and 1,5-benzodiazepine (7a-e). These were derived from chalcone (4a-e), showing improved pharmacological profiles. The compounds underwent characterization by FTIR, NMR, and Mass Spectroscopy, and their antimicrobial activities, along with structure-activity relationships (SAR), were assessed using in silico and in vitro methods.
View Article and Find Full Text PDFEur J Med Chem
January 2025
State Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources, Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources (Ministry of Education of China), Collaborative Innovation Center for Guangxi Ethnic Medicine, School of Chemistry and Pharmaceutical Sciences of Guangxi Normal University, Guilin, 541004, China; National & Local Joint Engineering Research Center for Mineral Salt Deep Utilization, Institute of Green Chemistry and Process Enhancement Technology, Huaiyin Institute of Technology, Huai'an, 223003, China. Electronic address:
Nowadays, hybrid molecule with dual targets activity or effect is regarded as an effective strategy for combating the drug resistance development in cancer therapy. Herein, novel of bifunctional conjugates targeting tubulin and MMPs inhibitors were synthesized. Among them, 15j exhibited robust anticancer activity in vitro and in vivo, with IC values of 0.
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