Testosterone acetate thiosemicarbazone (TATSC, 17-beta-hydroxyandrost-4-one acetate thiosemicarbazone) was synthesized and characterized by single crystal X-ray structure determination. The copper and platinum complexes of this steroid derivative were synthesized and characterized by spectroscopy and electrochemiatry. The in vitro activity of these compounds against human breast cancer cell line MCF-7 was tested. The highest activity was found for the [Pt(TATSC)Cl(1)] followed by [Cu(TATSC)Cl(2)] and the ligand in compariosn with cisplatin.
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http://dx.doi.org/10.1155/MBD.1999.177 | DOI Listing |
Sci Rep
December 2024
Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran.
In this work, a novel series of quinoline-thiosemicarbazone-1,2,3-triazole-aceamide derivatives 10a-n as new potent α-glucosidase inhibitors was designed, synthesized, and evaluated. All the synthesized derivatives 10a-n were more potent than acarbose (positive control). Representatively, (E)-2-(4-(((3-((2-Carbamothioylhydrazineylidene)methyl)quinolin-2-yl)thio)methyl)-1H-1,2,3-triazol-1-yl)-N-phenethylacetamide (10n), as the most potent entry, with IC = 48.
View Article and Find Full Text PDFFuture Med Chem
July 2024
Department of Chemistry, Faculty of Science, Arish University, Arish, 45511, Egypt.
Novel thiazole hybrids were synthesized via thiazolation of 4-phenylthiosemicarbazone (). The anticancer activity against the NCI 60 cancer cell line panel. Methyl 2-(2-((1-(naphthalen-2-yl)ethylidene)hydrazineylidene)-4-oxo-3-phenylthiazolidin-5-ylidene)acetate () showed significant anticancer activity at 10 μM with a mean growth inhibition (GI) of 51.
View Article and Find Full Text PDFSaudi Pharm J
December 2023
Department of Chemistry, Abdul Wali Khan University, Mardan 23200, Pakistan.
Background: Novel α-amylase inhibitors play a crucial role in managing diabetes and obesity, contributing to improved public health by addressing these challenging and prevalent conditions. Moreover, the synthesis of anti-oxidant agents is essential due to their potential in combating oxidative stress-related diseases and promoting overall health.
Objective: Synthesis of thoisemicarbazone derivatives of 2,4-dichlorophenyl acetic acid and to screened them for their biological activities.
ACS Omega
February 2023
Department of Pharmacy, University of Malakand, Dir Lower, Chakdara, Khyber Pakhtunkhwa18800, Pakistan.
The current research reports the synthesis of 14 para-substituted thiosemicarbazone derivatives in good to excellent yields using standard procedures. Initially, 4-ethoxybenzaldehyde () and 4-nitrobenzaldehyde () were refluxed with thiosemicarbazide in the presence of acetic acid in ethanol for 4-5 h. Then, various substituted phenacyl bromides were treated with the desired thiosemicarbazones ( and ) in the presence of triethylamine in ethanol with constant stirring for 5-6 h.
View Article and Find Full Text PDFRecent Adv Inflamm Allergy Drug Discov
January 2023
Computational Chemistry Research Lab, Department of Pharmaceutical Chemistry, Bharati Vidyapeeth College of Pharmacy, Kolhapur, 416013 Maharashtra, India.
Background: Recently, researchers have worked on the development of new methods for the synthesis of bioactive heterocycles using polyethylene glycol as a green solvent. In this context, we report the synthesized 2-(2-hydrazinyl) thiazoles for their in vitro antioxidant, in vitro anti-inflammatory and in vitro anti-cancer activities.
Objective: The objective of the study was to develop novel antioxidant, anti-inflammatory and anti-cancer drugs.
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