7546-52-3Relevant articles and documents
Design, synthesis, and spectroscopic study of 7-azaindolyl hydrazones with anti-breast cancer activity
Dongare, Sakharam B.,Bandgar, Babasaheb P.,Bhale, Pravin S.,Shringare, Sadanand N.,Chavan, Hemant V.
, p. 1 - 9 (2019/06/24)
A series of 7-azaindolyl hydrazones were prepared by reacting of hydrazides of 7-azaindole-3-acetic acids with aromatic aldehydes and N-substituted indolyl-3-carboxyaldehydes. Structure of all the synthesized compounds were satisfactorily correlated by IR, 1H NMR, 13C NMR and mass spectroscopic evidences. The synthesized compounds were evaluated for their possible anticancer potential against MCF-7 induced breast carcinoma. It is worth mentioning that most of the compounds were considerably active against MCF-7 cell line with GI50 values ranging from 22.3–81.0 μM. The hydrazones of N-1-substituted indole-3-carboxyaldehydes 9f, 9g, 9h, 9c, and 9j were active against MCF-7 cell line with GI50 values less than 40 μM (GI50 = 22.3 and 24.9, 29.6, 30.2 and 37.8 μM respectively) with moderate TGI values (TGI = 56.6, 59.5, 65.5, 70.7 and 94.6 μM respectively). The active compounds were also screened against the normal Vero monkey cell line, which showed moderate selectivity against inhibition of cancer cells.
Discovery and characterization of NVP-QAV680, a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases
Sandham, David A.,Arnold, Nicola,Aschauer, Heinrich,Bala, Kamlesh,Barker, Lucy,Brown, Lyndon,Brown, Zarin,Budd, David,Cox, Brian,Docx, Cerys,Dubois, Gerald,Duggan, Nicholas,England, Karen,Everatt, Brian,Furegati, Marcus,Hall, Edward,Kalthoff, Frank,King, Anna,Leblanc, Catherine J.,Manini, Jodie,Meingassner, Josef,Profit, Rachael,Schmidt, Alfred,Simmons, Jennifer,Sohal, Bindi,Stringer, Rowan,Thomas, Matthew,Turner, Katharine L.,Walker, Christoph,Watson, Simon J.,Westwick, John,Willis, Jennifer,Williams, Gareth,Wilson, Caroline
supporting information, p. 6582 - 6591 (2013/10/22)
Optimization of a 7-azaindole-3-acetic acid CRTh2 receptor antagonist chemotype derived from high throughput screening furnished a highly selective compound NVP-QAV680 with low nM functional potency for inhibition of CRTh2 driven human eosinophil and Th2 lymphocyte activation in vitro. The molecule exhibited good oral bioavailability in the rat, combined with efficacy in rodent CRTh2-dependent mechanistic and allergic disease models and was suitable for clinical development.