38204-31-8Relevant academic research and scientific papers
CONTINUOUS FLOW SYNTHESIS OF DITHIOESTER COMPOUNDS
-
Paragraph 0106, (2014/10/04)
The present technology relates to methods of producing various dithioester-containing compounds via continuous flow reactors.
Bioactivity of novel transition metal complexes of N′-[(4-methoxy)thiobenzoyl]benzoic acid hydrazide
Shrivastav, Anuraag,Tripathi, Pratibha,Srivastava, Ajay K.,Singh, Nand K.,Sharma, Rajendra K.
, p. 577 - 583 (2008/09/19)
Cu(II), Fe(III), and Mn(II) complexes of a novel ligand N′-[(4-methoxy)thiobenzoyl]benzoic acid hydrazide (H2mtbh) have been synthesized and characterized by elemental analyses, IR, UV-vis, NMR, mass, EPR and Moessbauer spectroscopy. The results suggest a square planar structure for [Cu(Hmtbh)Cl] and [Cu(mtbh)] whereas an octahedral structure for [Mn(Hmtbh)2] and [Fe(Hmtbh)(mtbh)]. Mn(II) and Fe(III) complexes were found to inhibit proliferation of HT29 cells. [Mn(Hmtbh)2] and [Fe(Hmtbh)(mtbh)] inhibited proliferation of HT29 cells with half maximal inhibition (IC50) of 8.15 ± 0.87 and 68.1 ± 4.8 μM, respectively, whereas H2mtbh showed growth inhibition with IC50 of 90.9 ± 7.8 μM and were able to inhibit NMT activity in vitro. Mn(II) and Fe(III) complexes inhibited NMT activity in a dose dependent manner with IC50 values of 20 ± 2.2 and 60 ± 7.2 μM, respectively, whereas ligand (H2mtbh) displayed IC50 of 3.2 ± 0.5 mM.
5′-Phenyl-3′H-spiro[indoline-3,2′-[1,3,4]thiadiazol]-2-one inhibitors of ADAMTS-5 (Aggrecanase-2)
Bursavich, Matthew G.,Gilbert, Adam M.,Lombardi, Sabrina,Georgiadis, Katy E.,Reifenberg, Erica,Flannery, Carl R.,Morris, Elisabeth A.
, p. 5630 - 5633 (2008/03/14)
5′-Phenyl-3′H-spiro[indoline-3,2′-[1,3,4]thiadiazol]-2-one inhibitors of ADAMTS-5 (Aggrecanase-2) have been prepared via commercially available starting materials. Selected compounds 23, 33-35 show sub-micromolar ADAMTS-5 potency and strong SAR trends with selectivity over the related metalloproteases ADAMTS-4 (Aggrecanase-1), MMP12, and MMP13. This series of compounds represents progress toward a selective ADAMTS-5 inhibitor as a disease modifying osteoarthritis drug.
