1013-93-0Relevant academic research and scientific papers
Inactivation of the human papillomavirus-16 E6 oncoprotein by organic disulfides
Beerheide, Walter,Sim, Mui Mui,Tan, Yee-Joo,Bernard, Hans-Ulrich,Ting, Anthony E
, p. 2549 - 2560 (2000)
We are investigating compounds that could be useful in the treatment of neoplastic lesions of the cervix by acting on the oncoprotein E6 of human papillomavirus-16. The E6 protein contains two potential zinc-binding domains that are required for most of its functions. We have published tests that measure (i) the release of zinc ions after chemical alteration of the cysteine groups of these zinc-binding domains (TSQ assay), (ii) the interaction of E6 with the cellular proteins E6AP and E6BP (BIACORE assay), and (iii) the viability of tumor cell lines that require the continuous expression of HPV oncoproteins (WST1 assay). Based on these tests, we identified 4,4'-dithiodimorpholine as a potential lead compound. In this study we examined whether the dithiobisamine moiety of 4,4'-dithiodimorpholine may be an important molecular prerequisite for further drug development in this system. We have evaluated 59 new substances including organic disulfides and those containing the dithiobisamine moiety, as well as structural analogues. The compounds with significant reactivity in all three assays were observed only for dithiobisamine derivatives with saturated cyclic amines and aryl substituted piperazines. The identity of these substances suggests that the N-S-S-N moiety is necessary but not sufficient for reactivity in our assays, and that dithiobisamine based substances are useful as lead compounds that target the cysteine groups of HPV-16 E6 zinc fingers. Copyright (C) 2000 Elsevier Science Ltd.
THERMAL DECOMPOSITION OF TRIS(N,N-DISUBSTITUTED DITHIOCARBAMATE) COMPLEXES OF As(III), Sb(III) AND Bi(III).
Lalia-Kantouri,Manoussakis
, p. 1151 - 1169 (2008/10/08)
Thermal studies on tris(N,N-disubstituted dithiocarbamates) of arsenic(III), antimony(III) and bismuth(III) of the type M left bracket S//2CX right bracket //3 (M equals As, Sb, Bi; X equals NEt//2, N(CH//2)//4O) by simultaneous TG, DTG and DTA were carried out in air and nitrogen atmospheres. The apparent activation energies were determined by the graphical method of Freeman-Carroll, modified for n equals 1, and Piloyan's two methods from the TG and DTG curves. The TTN temperatures were calculated from the TG profiles. A possible mechanism of the decomposition reaction is suggested on the basis of the results of their pyrolysis and their mass spectral data. The intermediates obtained at the ends of various decomposition stages were identified via elemental analysis and i. r. and mass spectral data, whereas the residues were identified by X-ray powder diffraction analysis.
