26648-11-3

Upstream product

• 75-15-0 carbon disulfide 

Downstream Products

• 13331-31-2 S-benzyldithiocarbazate 
• 5397-03-5 hydrazinecarbodithioic acid methyl ester 
• 1190854-47-7 ethyl 3-{[4-(2,6-dimethoxy-4-(methoxymethyl)phenyl]-2-thioxo-1,3-thiazole-3(2H)-yl]-amino}-3-oxopropanoate 
• 34930-16-0 hydrazinecarbodithioic acid 4-methoxy-benzyl ester 
• 1013035-58-9 C₈H₉FN₂S₂ 
• 73798-89-7 phenacyl hydrazinodithioformate 
• 471-32-9 dithiocarbonic acid hydrazide 

Relevant academic research and scientific papers

Antitumor activity of a novel dual functional podophyllotoxin derivative involved PI3K/AKT/ mTOR pathway

The progression of cancer through local expansion and metastasis is well recognized, but preventing these characteristic cancer processes is challenging. To this end, a new strategy is required. In this study, we presented a novel dual functional podophyl

A crystallographic study of S-methyl 2-(5-chloro-2-oxoindolin-3-ylidene) hydrazinecarbodithioate

S-methyl 2-(5-chloro-2-oxoindolin-3-ylidene)hydrazinecarbodithioate (SM5ClISA) has been prepared from S-methyldithiocarbazate and 5-chloroisatin. The compound crystallized in monoclinic crystal system with space group P 2 1/n, Z = 4, V = 1201.85(7) A3 and unit cell parameters a = 6.5466(2) A, b = 7.5056(3) A, c = 24.6509(8) A, α = γ = 90° and β = 97.1434(18)°. The crystal structure reveals that the compound exists in the thione form with the chlorine occupies the fifth position in the isatin ring with the bond length of 1.739(2) A. The 5-chloroisatin moiety is trans with respect to the C3-N2 and C3-S4 bonds whereas the methyl group of the dithiocarbazate moiety is cis with respect to the C3-N2 and C3-S5 bonds.

Copper ion attenuated the antiproliferative activity of di-2-pyridylhydrazone dithiocarbamate derivative; however, there was a lack of correlation between ROS generation and antiproliferative activity

The use of chelators for cancer treatment has been an alternative option. Dithiocarbamates have recently attracted considerable attention owning to their diverse biological activities; thus, the preparation of new dithiocarbamate derivatives with improved antitumor activity and selectivity as well as probing the underlying molecular mechanism are required. In this study, di-2-pyridylhydrazone dithiocarbamate S-propionic acid (DpdtpA) and its copper complex were prepared and characterized, and its antiproliferative activity was evaluated. The proliferation inhibition assay showed that DpdtpA exhibited excellent antiproliferative effect in hepatocellular carcinoma (IC50 = 1.3 ± 0.3 μM for HepG2, and 2.5 ± 0.6 μM for Bel-7402). However, in the presence of copper ion, the antiproliferative activity of DpdtpA was dramatically attenuated (20-30 fold) owing to the formation of copper chelate. A preliminarily mechanistic study revealed that reactive oxygen species (ROS) generation mediated the antiproliferative activity of DpdtpA, and accordingly induced apoptosis, DNA cleavage, and autophagy. Surprisingly, the cytotoxicity of DpdtpA copper complex (DpdtpA-Cu) was also involved in ROS generation; however, a paradoxical relation between cellular ROS level and cytotoxicity was observed. Further investigation indicated that DpdtpA could induce cell cycle arrest at the S phase; however, DpdtpA-Cu lacked this effect, which explained the difference in their antiproliferative activity.

Synthesis, characterization and bioactivity studies of new dithiocarbazate complexes

A new compound of the dithiocarbazate family, 2,2′-((disulfanediylbis((ethylthio)methylene))bis(hydrazin-2-yl-1-ylidene))bis(2-oxo-1,2-dihydro-3H-indol-3-ylidene), and its five metal complexes are synthesized. All compounds are characterized by elemental and mass analysis, spectroscopic (FT-IR,1H-NMR and13C-NMR) and TGA techniques. The crystal structure of the synthesized compounds is determined by single crystal X-ray diffraction analysis, which shows that the ligand acts as a tridentate chelate coordinated to Zn, Co and Ni ions in a distorted octahedral fashion and also as bidentate to Pt and Pd ions in a distorted square planar geometry. In order to investigate the compounds’ cytotoxicity, two human cancer cell lines of HeLa and MCF-7 are used and compared to the normal cell line of CHO. The clinical drug cisplatin is used as the standard drug. Fluorescence spectrophotometry is used to study the interaction of the compounds with human serum albumin (HSA) and parameters such as the Stern-Volmer quenching constant (KSV), the number of binding sites (n), association constants (Ka) and free energy changes (ΔG) at 298 K are calculated.

Novel Cu(II) Schiff Base Complex Combination with Polymyxin B/Phenylalanine-Arginine β-Naphthylamide Against Various Bacterial Strains

Concerns on increasing trends of multidrug resistance (MDR) around the world have triggered the need to investigate and develop new therapeutic strategies and potent antibacterial drugs. Polymyxins, a class of polycationic antimicrobial peptides, have been regarded as the last-line therapy against Gram-negative bacteria due to limited new antibiotics and phenylalanine-arginine β-naphthylamide (PAβN), a peptidomimetic compound has been characterised as an efflux pump inhibitor (EPI) that have been investigated to overcome efflux-mediated multidrug resistance. In this work, the antibacterial activity of two Schiff base ligands derived from the condensation of S-benzyl dithiocarbazate with 4-carboxybenzaldehye (SB4CB) and 4-formyl-3-hydroxybenzoic acid (SBFH) their copper(II) complexes (Cu(SB4CB)2 and Cu(SBFH)2) were tested individually, and the most promising compound was tested in combination with polymyxin B (POLY) and PAβN against different bacteria, such as antibiotic-susceptible strains: Acinetobacter baumannii ATCC 19606, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853, and Staphylococcus aureus ATCC 35923; multidrug-resistant strains: A. baumannii ATCC BAA-1797, E. coli BAA-196, P. aeruginosa ATCC BAA-2108 and S. aureus ATCC 43300. Initial minimum inhibition concentration (MIC) results showed the Cu(II) complexes Cu(SB4CB)2 and Cu(SBFH)2, demonstrated obvious antibacterial activity as compared to the ligand alone. Fractional inhibitory concentration (FIC) index showed improved MIC values with additivity and synergistic effect for Cu(SBFH)2 in combination with POLY and PAβN. From the in silico molecular docking investigation, Cu(SBFH)2 was shown to engage in hydrophobic interactions via its phenyl rings with surrounding hydrophobic residues in the binding pocket of S. aureus NorA, E. coli AcrB, P. aeruginosa MexB and A. baumannii AdeB efflux pumps. The phenyl rings of the ligand could also form π-π stacking with adjacent residues in the binding site of A. baumannii AdeB. Besides, hydrogen bonding and π-cation interactions were also observed via the carboxyl group, hydroxyl group and phenyl ring of SBFH moiety, respectively with nearby residues in the E. coli AcrB binding pocket. This study indicates that the combination strategy of Cu(SBFH)2 with POLY and PAβN enhances therapeutic potential and sheds light on the binding pockets inside bacteria efflux pumps and the binding interactions of ligand in the binding site.

Synthesis, characterization and pioactivity study of bidentate NS schiff base of S-Benzyl dithiocarbazate and its Zn(II) and Pd(II) complexes

The bis-chelated four coordinate complexes (ML2, L = deprotonated ligand) of Zn(II) and Pd(II) ions were synthesized, derived from a new bidentate NS Schiff base called S-benzyl-β-N-(4-hydroxy-3-nitrophenyl)methylene dithiocarbazate (HL) which is the condensation product of S-benzyl dithiocarbazate (SBDTC) with 4-hydroxy-3-nitrobenzaldehyde. The synthesized ligand and complexes were characterized using conventional techniques like NMR, UV-visible, IR, mass spectroscopic techniques, magnetic susceptibility measurement and molar conductance. A single crystal X-ray crystallography data approved the proposed crystal structure of the ligand. Both in solid and solution phase, the ligand continues to exist in its thione tautomeric form. The chelates were formed by the reaction of ligand with the metal ions through the ligand azomethine nitrogen atom and the deprotonated thiolate sulfur anion. Magnetic susceptibility and electronic spectroscopic data suggested to have a tetrahedral geometry for ZnL2 complex whereas a square planar structure for PdL2 complex. The analgesic and anti-inflammatory bioactivity were assayed on both the ligand and its complexes by tail flick and carrageenan induced paw edema test. The ligand at the dose of 10 mg/kg, produced a significant (p 0.001) increase in pain threshold in tail flick methods when compared to control but in case of complexes, it showed moderate activity. At the same dose, the ligand and complexes significantly (p 0.001) reduced paw edema when compared to the control. Altogether, these results suggest that ligand and its complexes could be used as a potent anti-inflammatory agent.

OXADIAZOLE LINKERS AND USE THEREOF

Provided is oxadiazole linkers and use thereof, more specifically to the compounds represented by formulas (I), (II), and (III), and their use in the preparation of antibody-drug conjugates (ADCs). The ADCs obtained from said oxadiazole linkers have high homogeneity and stability, and could be used effectively for the treatment of various diseases including tumors. The definition of the groups in formula (I), (II), and (III) is the same as that in the description.

Synthesis and pesticidal activities of novel anthranilic diamides containing pyridylpyrazole and iminodithiocarbamate or thiosemicarbazone motifs

A series of novel anthranilic diamide derivatives containing pyridylpyrazole and iminodithiocarbamate or thiosemicarbazone motifs were synthesized via multi-step reactions. The structures of seven title compounds (methyl 2-(2-(3-bromo-1-(3-chloropyridin-2-yl)-1H-pyrazole-5-carboxamido)-5-chloro-3- methylbenzylidene)hydrazinecarbodithioate 7 and 3-bromo-N-(2-((2-substitutedcarbamothioylhydrazono)methyl)-4-chloro-6-methylphenyl)-1-(3-chloropyridin-2-yl)-1H-pyrazole-5-carboxamide 8a-8f) were confirmed by melting points, IR, 1H NMR, 13C NMR, and HRMS. The bioassays showed that some of the compounds exhibited modest insecticidal activities against oriental armyworm (Mythimna separata Walker), particularly, compound 8b (3-bromo-N-(4-chloro-2-methyl-6-((2-(methylcarbamothioyl)hydrazono)methyl)phenyl)-1-(3-chloropyridin-2-yl)-1H-pyrazole-5-carboxamide) held 100% and 30% larvicidal activity at the concentration of 25 mg/L and 10 mg/L, respectively. In addition, several compounds displayed favorable fungicidal activities against Alternaria solani Sorauer and Physalospora piricola at 50 μg/mL, and were comparable with the controls Chlorothalonil and Triadimefon. The results in this paper will provide important information for further research and development of sulfur-containing heterocyclic agrochemicals.

Dithiocarbamic acid derivative, and preparation method and application thereof

The invention discloses a dithiocarbamic acid derivative, and a preparation method and an application thereof. A novel dithiocarbamic acid derivative is synthesized according to the invention and has new biological characteristics that (1) the growth of liver cancer, colon cancer and ovarian carcinoma cells can be restrained and the median inhibitory concentration is low; (2) the vascularization can be restrained under low concentration condition and the cancer cell metastasis can be restrained; (3) the cytotoxicity is related to apoptosis-inducing, cycle arrest and autophagy.

BCR-ABL TYROSINE-KINASE LIGANDS CAPABLE OF DIMERIZING IN AN AQUEOUS SOLUTION, AND METHODS OF USING SAME

Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. invivo) to form a multimer (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding sites on a Bcr-Abl tyrosine kinase.