1062259-61-3Relevant articles and documents
Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen
Cheeseman, Matthew D.,Chessum, Nicola E. A.,Rye, Carl S.,Pasqua, A. Elisa,Tucker, Michael J.,Wilding, Birgit,Evans, Lindsay E.,Lepri, Susan,Richards, Meirion,Sharp, Swee Y.,Ali, Salyha,Rowlands, Martin,O’Fee, Lisa,Miah, Asadh,Hayes, Angela,Henley, Alan T.,Powers, Marissa,Te Poele, Robert,De Billy, Emmanuel,Pellegrino, Loredana,Raynaud, Florence,Burke, Rosemary,Van Montfort, Rob L. M.,Eccles, Suzanne A.,Workman, Paul,Jones, Keith
, p. 180 - 201 (2017/04/26)
Phenotypic screens, which focus on measuring and quantifying discrete cellular changes rather than affinity for individual recombinant proteins, have recently attracted renewed interest as an efficient strategy for drug discovery. In this article, we describe the discovery of a new chemical probe, bisamide (CCT251236), identified using an unbiased phenotypic screen to detect inhibitors of the HSF1 stress pathway. The chemical probe is orally bioavailable and displays efficacy in a human ovarian carcinoma xenograft model. By developing cell-based SAR and using chemical proteomics, we identified pirin as a high affinity molecular target, which was confirmed by SPR and crystallography.
Synthesis of aminoquinazoline derivatives and their antiproliferative activities against melanoma cell line
Lee, Junsang,Nam, Bong Soo,Kim, Hwan,Oh, Chang-Hyun,Lee, So Ha,Cho, Seung Joo,Sim, Tae Bo,Hah, Jung-Mi,Kim, Dong Jin,Tae, Jinsung,Yoo, Kyung Ho
scheme or table, p. 5722 - 5725 (2010/11/24)
The synthesis of a novel series of aminoquinazoline derivatives 1a-r and their antiproliferative activities against A375 human melanoma cell line were described. Among them, six compounds showed superior antiproliferative activities to Sorafenib as a reference compound. In particular, the representative compound 1q bearing chromen-4-one moiety exhibited excellent antiproliferative activity (IC50 = 0.006 μM) and good selectivity over HS27 fibroblast cell line.
