502491-87-4

Upstream product

• 2144-08-3 2,3,4-trihydroxybenzylaldehyde 
• 5351-69-9 4-Phenyl-3-thiosemicarbazide 
• 103-72-0 phenyl isothiocyanate 

Downstream Products

• 1459803-53-2 C₁₉H₁₇N₃O₃S*BrH 
• 1459803-84-9 C₁₇H₁₅N₃O₃S*ClH 

Relevant academic research and scientific papers

Nickel(II) Complexes with Polyhydroxybenzaldehyde and O,N,S tridentate Thiosemicarbazone ligands: Synthesis, Cytotoxicity, Antimalarial Activity, and Molecular Docking Studies.

A series of Schiff base metal complexes with the formulations [Ni(L1)PPh3]Cl (1), [Ni(L2)PPh3]Cl (2), [Ni(L3)PPh3] (3), and [Ni(L4)PPh3] (4) (where L1 = 2,3,4-trihydroxybenzaldehyde-4-methyl-3-thiosemicarbazone,

Synthesis and characterization of newly synthesized thiosemicarbazone ligands with IR, NMR and mass spectral techniques

Among various organic chelating agents thiosemicarbazones occupy an important role due to their efficiency towards many metal ions through thionate sulphur atom and hydrazino nitrogen atom. Thiosemicarbazones can be obtained by condensing thiosemicarbazid

Structural revision of the Mcl-1 inhibitor MIM1: synthesis and biological studies on ovarian cancer cells with evaluation of designed analogues

In the area of cancer research, the development of new and potent inhibitors of anti-apoptotic proteins is a very active and promising topic. The small molecule MIM1 has been reported earlier as one of the first selective inhibitors of the anti-apoptotic protein Mcl-1. In the present paper, we first revised the structure of this molecule based on extensive physicochemical analyses. Then we designed and synthesized a focused library of analogues for the corrected structure of MIM1. Next, these molecules were subjected to a panel ofin cellulobiological studies, allowing the identification of dual Bcl-xL/Mcl-1 inhibitors, as well as selective Mcl-1 inhibitors. These results have been complemented by fluorescence polarization assays with the Mcl-1 protein. Preliminary structure-activity relationships were discussed and extensive molecular modelling studies allowed us to propose a rationale for the biological activity of this series of new inhibitors, in particular for the selectivity of inhibition of Mcl-1versusBcl-xL

INHIBITION OF MCL-1 AND/OR BFL-1/A1

This disclosure features compounds and pharmaceutically acceptable salts thereof that inhibit MCL-1 and/or BFL-1/A1 and compositions containing the same. This disclosure also features combinations that include one or more of the MCL-1/BFL-1/A1 inhibitor compounds described herein, or a pharmaceutically acceptable salt thereof; and one or more additional therapeutic agents (e.g., one or more chemotherapeutic agents (including small molecule and/or anti-body based chemotherapy and/or radiation); e.g., one or more therapeutic agents that modulate apoptosis; e.g., one or more therapeutic agents that bind to and inhibit anti-apoptotic proteins or modulate them indirectly; e.g., one or more therapeutic agents that bind to and inhibit, or indirectly modulate, anti-apoptotic BCL-2, BCL-XL, BCL-w, MCL-1, and/or BFL-1/A1; e.g., one or more therapeutic agents that directly bind to and inhibit anti-apoptotic BCL-2 / BCL-XL; e.g., agents such as ABT-199, ABT-263 and ABT-737; e.g., ABT-737), or (where applicable) a pharmaceutically acceptable salt of the one or more therapeutic agents (as well as compositions containing the same). Also featured are methods of using such compounds, salts, combinations, and compositions, e.g., for the treatment or prevention of diseases, disorders, and conditions associated with deregulated apoptosis of cells (e.g., diseased or damaged cells; e.g., insufficient apoptosis of diseased or damaged cells or reduced apoptosis of diseased or damaged cells)..

Evaluating anti-Toxoplasma gondii activity of new serie of phenylsemicarbazone and phenylthiosemicarbazones in vitro

While Toxoplasma gondii is able to infect and replicate within all eukaryotic cells, tachyzoites are the infective form of T. gondii that invades all eukaryotic cells leading to tissue rupture, the main features of toxoplasmosis. The present study evaluates the activity of (benzaldehyde)-4- phenyl-3-thiosemicarbazone and (benzaldehyde)-(4 or 1)-phenylsemicarbazone against intracellular T. gondii. The nine new compounds were incubated in infected Vero cells at concentrations of 0.01, 0.1, 0.5, and 1.0 mM and evaluated for three main effects: cytotoxicity, infection, and number of intracellular parasites. The cytotoxicity test showed a pattern by analyzing the substituent arylhydrazone, where trihydroxy Compounds 4-9 were cytotoxic at concentrations of 0.5 and 1.0 mM. The results highlight Compound 8, which reduced the number of intracellular parasites by 82 % in a concentration of 0.01 mM and showed a LD50 of 0.3 mM in cell culture. These different biological actions are due to changes in the molecular structure and type of radical present in each compound. All compounds tested were more efficient than the control drug sulfadizine.