142142-23-2Relevant academic research and scientific papers
Discovery of protein-protein interaction inhibitors of replication protein A
Patrone, James D.,Kennedy, J. Phillip,Frank, Andreas O.,Feldkamp, Michael D.,Vangamudi, Bhavatarini,Pelz, Nicholas F.,Rossanese, Olivia W.,Waterson, Alex G.,Chazin, Walter J.,Fesik, Stephen W.
, p. 601 - 605 (2013/07/26)
Replication protein A (RPA) is a ssDNA binding protein that is essential for DNA replication and repair. The initiation of the DNA damage response by RPA is mediated by protein-protein interactions involving the N-terminal domain of the 70 kDa subunit with partner proteins. Inhibition of these interactions increases sensitivity toward DNA damage and replication stress and may therefore be a potential strategy for cancer drug discovery. Toward this end, we have discovered two lead series of compounds, derived from hits obtained from a fragment-based screen, that bind to RPA70N with low micromolar affinity and inhibit the binding of an ATRIP-derived peptide to RPA. These compounds may offer a promising starting point for the discovery of clinically useful RPA inhibitors.
In vitro antifungal activity of some new triazole compounds
Chanda, Sumitra,Baluja, Shipra,Parekh, Jigna
, p. 281 - 285 (2012/11/07)
In the present study, the derivatives of 1,2,4-triazoles were synthesized and tested for antifungal activity against Candida tropicalis ATCC-4563, Candida albicans ATCC-2091, Cryptococcus neoformans ATCC-34664, Trichosporon beigelii NCIM-3404 and Aspergillus flavus NCIM-538 by disc diffusion method. 1,2,4-Triazoles were obtained by cyclization of the potassium salt of substituted dithiocarbazinic acid with hydrazine hydrate. The new synthesized compounds were characterized using IR, 1H NMR spectral data and Mass spectrometry together with elemental analysis. The inhibitory effect of the newly synthesized triazole compounds was compared to the standard antifungal agents. Minimum inhibitory concentration (MIC) was determined for those compounds which could inhibit all the tested fungal strains with maximum inhibition zone.
