106010-23-5

Upstream product

• 79-19-6 thiosemicarbazide 
• 93-55-0 1-phenyl-propan-1-one 

Downstream Products

• 113720-23-3 copper(II) propiophenone thiosemicarbazone 
• 113720-24-4 Pd(propiophenone thiosemicarbazone)2 
• 113720-25-5 Pt(propiophenone thiosemicarbazone)2 
• 113720-16-4 Ni(propiophenone thiosemicarbazone)2(pyridine)2 
• 113720-22-2 Ni(propiophenone thiosemicarbazone)2 
• 113720-17-5 Cu(propiophenone thiosemicarbazone)2(pyridine)2 
• 113720-21-1 Co(propiophenone thiosemicarbazone)2 
• 5213-43-4 [4-oxo-2-(1-phenyl-propylidenehydrazono)-thiazolidin-5-yl]-acetic acid 

Relevant academic research and scientific papers

Synthesis and pharmacological screening of a large library of 1,3,4-thiadiazolines as innovative therapeutic tools for the treatment of prostate cancer and melanoma

Antimitotic agents are widely used in cancer chemotherapy but the numerous side effects and the onset of resistance limit their clinical efficacy. Therefore, with the purpose of discovering more selective and efficient anticancer agents to be administered alone or in combination with traditional drugs, we synthesized a large library of 1,3,4-thiadiazoline analogues, maintaining the pharmacophoric structure of an antiproliferative compound known as K858: this is a new inhibitor of kinesin Eg5, able to induce the mitotic arrest in colorectal cancer cells and in xenograft ovarian cancer cells. We screened 103 compounds to assess their antiproliferative activity on PC3 prostate cancer cell line. Two derivatives, compounds 32 (corresponding to K858) and 33, have shown to be the most effective against prostate tumor cells and also towards two melanoma cell lines (SK-MEL-5 and SK-MEL-28) at low micromolar concentrations, confirming the pharmacological activity of this scaffold and revealing the potential role of 1,3,4-thiadiazolines in the management of cancer.

M-STAGE KINESIN INHIBITOR

A mitotic kinesin Eg5 inhibitor which comprises a thiadiazoline derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein R1 represents a hydrogen atom and the like, R2 represents a hydrogen atom, -C(=W)R6 (wherein W represents an oxygen atom or a sulfur atom, and R6 represents substituted or unsubstituted lower alkyl and the like) and the like, R3 represents -C(=Z)R19 (wherein Z represents an oxygen atom or a sulfur atom, and R19 represents substituted or unsubstituted lower alkyl and the like) and the like, R4 represents substituted or unsubstituted lower alkyl and the like, and R5 represents substituted or unsubstituted aryl and the like] and the like are provided.

THIADIAZOLINE DERIVATIVE

(wherein R1 and R4 are the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkynyl, substituted or unsubstituted lower alkenyl, or the like; R5 represents a substituted or unsubstituted heterocyclic group, substituted or unsubstituted aryl, or the like; R2 represents -C(-W)R6 or the like; R3 represents a hydrogen atom, -C(=WA)R6A, or the like) Antitumor agents which comprises a thiadiazoline derivative represented by the aforementioned general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient are provided.

New cyclometallated platinum(II) compounds with thiosemicarbazones: Crystal and molecular structure of [Pt{4-MeC6H3C(Me)=NN=C(S)NH2}(PPh3)]

Treatment of the thiosemicarbazones 3-CH3(CH2)5OC6H 4C(Me)=NN(H)C(=S)NH2 (a), 4-MeC6H4C(Me)=NN(H)=C(S)NH2 (b), C6H5C(Et)=NN(H)=C(S)NH2 (c), C6H5C{CH3(CH2) 10}=NN(H)=C(S)NH2 (d) and 4-MeC6H4C(Me)=NN(H)=C(S)NHMe (e) with K2[PtCl4] gives tetranuclear platinum(II) compounds 1a-1e with deprotonation of the -NH- group and with the ligand acting as a terdentate [C,N,S] moiety. Reaction of 1a-1e with PPh3 and of 1a with P(4-MeOC6H4)3 yielded mononuclear species 2a-2e and 3a, respectively. Treatment of 1a with the diphosphines Ph2PCH2PPh2 (dppm), Ph2P(CH2)2PPh2 (dppe), Ph2P(CH2)3PPh2 (dppp), Ph2P(CH2)4PPh2 (dppb), Ph2P(CH2)5PPh2 (dpppe), Ph2P(CH2)6PPh2 (dpph), and 1,1′-ferrocenebis(diphenylphosphine) (dppf) gives dinuclear compounds 4a-10a. In all cases the Pd-Schelating bond is strong enough to withstand reaction with the phosphorus ligands without bond cleavage. The molecular structure of 2b has been determined by X-ray crystallography. Mononuclear units are held together by hydrogen bonding, forming dimers in the solid state.