74959-63-0

Upstream product

• 83639-13-8 2,4-bis(4-methylphenyl)-3-azabicyclo[3.3.1]nonan-9-one 
• 5351-69-9 4-Phenyl-3-thiosemicarbazide 
• 108-94-1 cyclohexanone 
• 104-87-0 4-methyl-benzaldehyde 
• 103-72-0 phenyl isothiocyanate 

Downstream Products

• 74959-56-1 5-(4-methylphenyl)-N-phenyl-2-amino-1,3,4-thiadiazole 
• 98178-24-6 4-methyl-benzaldehyde (4-oxo-3-phenyl-thiazolidin-2-ylidene)-hydrazone 
• 74959-56-1 phenyl-(5-p-tolyl-[1,3,4]thiadiazol-2-yl)-amine 

Relevant academic research and scientific papers

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

A thiosemicarbazone derivative induces triple negative breast cancer cell apoptosis: possible role of miRNA-125a-5p and miRNA-181a-5p

Background: Breast cancer, the most commonly diagnosed malignancy in women, accounts for the highest cancer-related deaths worldwide. Triple negative breast cancer (TNBC), lacking the expression of estrogen, progesterone and HER2 receptors, has an aggressive clinical phenotype and is susceptible to chemotherapy but not to hormonal or targeted immunotherapy. In an attempt to identify potent and selective anti-TNBC agents, a set of thiosemicarbazone derivatives were screened for their cytotoxic activity against MDA-MB 231 breast cancer cell line. Methods: MTT assay was used to examine cell viability. P53 phosphorylation status, poly (ADP-ribose) polymerase (PARP) cleavage as well as Bcl2 and Bax protein levels were assessed by Western blot. Quantitative Real Time-PCR was carried out to characterize miRNAs expression levels. Results: Combining Cisplatin + thiosemicarbazone compound 4 showed potent anti-TNBC potential. Cisplatin + compound 4 significantly enhanced p53 phosphorylation, induced Bax amount, reduced Bcl2 protein levels, enhanced PARP cleavage and modulated miRNAs expression profile in TNBCs, with a particular overexpression of miR-125a-5p and miR-181a-5p. Intriguingly, miR-125a-5p and miR-181a-5p could significantly downregulate BCL2 expression by binding to their target sites in the 3′UTR. Conclusions: Collectively, our results demonstrate an anti-TNBC activity of Cisplatin + thiosemicarbazone compound 4 combination mediated via induction of apoptosis.

Cd(II) complexes with two new ligands [2-thiophenecarboxaldehyde-4-phenylthiosemicarbazone and 4-methylbenzaldehyde-4-phenylthiosemicarbazone]: Synthesis, spectral characterization and thermogravimetric studies

Background: We synthesized two new organic chelating agents, such as 2-thiophene carboxaldehyde-4-phenylthiosemicarbazone (TCPTSC) and 4-methylbenzaldehyde-4-phenylthiosemicarbazone (MBP TSC) and applied to chelation with Cd(II). Both the ligands (TCPTSC

Synthesis and antimicrobial studies of novel 2,4-diaryl-3-azabicyclo[3.3.1] nonan-9-one 4′-phenylthiosemicarbazones

New series of 2,4-diaryl-3-azabicyclo[3.3.1]nonan-9-one 4′-phenylthiosemicarbazones (compounds 9-16) was obtained from the corresponding 2,4-diaryl-3-azabicyclo[3.3.1]nonan-9-ones. The synthesized compounds have been characterized by their elemental, anal