7411-05-4Relevant academic research and scientific papers
In vitro and in vivo anticancer activity of tridentate thiosemicarbazone copper complexes: Unravelling an unexplored pharmacological target
Carcelli, Mauro,Tegoni, Matteo,Bartoli, Jennifer,Marzano, Cristina,Pelosi, Giorgio,Salvalaio, Marika,Rogolino, Dominga,Gandin, Valentina
, (2020)
Certain metal complexes can have a great antitumor activity, as the use of cisplatin in therapy has been demonstrating for the past fifty years. Copper complexes, in particular, have attracted much attention as an example of anticancer compounds based on
A Series of Benzylidenes Linked to Hydrazine-1-carbothioamide as Tyrosinase Inhibitors: Synthesis, Biological Evaluation and Structure?Activity Relationship
Hosseinpoor, Hona,Iraji, Aida,Edraki, Najmeh,Pirhadi, Somayeh,Attarroshan, Mahshid,Khoshneviszadeh, Mahsima,Khoshneviszadeh, Mehdi
, (2020/08/05)
Tyrosinase is a type 3 copper enzyme responsible for skin pigmentation disorders, skin cancer, and enzymatic browning of vegetables and fruits. In the present article, 12 small molecules of 2-benzylidenehydrazine-1-carbothioamide were designed, synthesized and evaluated for their anti-tyrosinase activities followed by molecular docking and pharmacophore-based screening. Among synthesized thiosemicarbazone derivatives, one compound, (2E)-2-[(4-nitrophenyl)methylidene]hydrazine-1-carbothioamide, is the strongest inhibitor of mushroom tyrosinase with IC50 of 0.05 μM which demonstrated a 128-fold increase in potency compared to the positive control. Kinetic studies also revealed mix type inhibition by this compound. Docking studies confirmed the complete fitting of the synthesized compounds into the tyrosinase active site. The results underline the potential of 2-benzylidenehydrazine-1-carbothioamides as potent pharmacophore to extend the tyrosinase inhibition in drug discovery.
Investigation of the salicylaldehyde thiosemicarbazone scaffold for inhibition of influenza virus PA endonuclease
Rogolino, Dominga,Bacchi, Alessia,De Luca, Laura,Rispoli, Gabriele,Sechi, Mario,Stevaert, Annelies,Naesens, Lieve,Carcelli, Mauro
, p. 1109 - 1121 (2015/10/19)
The influenza virus PA endonuclease is an attractive target for the development of novel anti-influenza virus therapeutics, which are urgently needed because of the emergence of drug-resistant viral strains. Reported PA inhibitors are assumed to chelate t
Synthesis, biological assay in vitro and molecular docking studies of new Schiff base derivatives as potential urease inhibitors
Aslam, Muhammad Adil S.,Mahmood, Shams-Ul,Shahid, Mohammad,Saeed, Aamer,Iqbal, Jamshed
experimental part, p. 5473 - 5479 (2011/12/03)
A series of new and novel Schiff base derivatives were synthesized and investigated as potential new inhibitors of Jack bean urease. The most potent compounds were 3f with (Ki = 0.09 μM) and 3k (Ki = 0.122 μM). A pure competitive mec
