Synthesis and biological evaluation of novel pyrazole derivatives with anticancer activity

Gallium compounds in nuclear medicine and oncology

“…These are the radiopharmaceuticals employing radioactive 67,68 Ga(III) isotopes, e.g., Ga(imidazole)3 and its derivates, as epidermal growth factor receptors (Garcia et al, 2009); GaCl3, for imaging of lymphoma, inflammatory processes, transmitting nerve impulses, and regulatory fluid in and out of cells (Collery et al, 2000;Silvola et al, 2011); Ga-folate, as diagnostic agent for receptor-positive tumor (Melpomeni et al, 2011); Ga-citrate, suitable for scintigraphy for the detection of a wide variety of diseases: Hodgkin's, lung cancer, malignant lymphoma, and pancreatic cancer (Kunn et al, 1997;Liu et al, 2003;Lin et al, 2007); Ganitroimidazole and its derivative, for PET imaging of tumor hypoxia (Goldman, 1982;Juchau, 1989;Kunn et al, Brought to you by | University of Bath Authenticated Download Date | 6/13/15 1:16 AM 1997; Fernández et al, 2013); and Ga-biphosphonate, for PET tracing of bone lesions (Fellner et al, 2012). There are also some conventional pharmaceuticals employing nonradio active Ga(III) pharmaceuticals used in oncology, e.g., Ga-EDTMP, for therapy of bone metastasis (Su et al, 2005); Ga(8-quinolinate)3, for treating renal cell cancer (Collery et al, 2000;Jalilian et al, 2005;Rudnev et al, 2006); Ga-semicarbazones, with a wide spectrum of antitumor effects in the ovary, breast, and colon (Rudnev et al, 2006;Kalinowski et al, 2009;Gambino et al, 2011); Ga(maltol)3, for the treatment of several types of cancer, including liver cancer and lymphoma (Rudnev et al, 2006); Ga(nitrate)3, for the treatment of lymphomas, bone metastasis, and bladder cancer (Collery et al, 2002;Jakupec and Keppler, 2004); Ga-porphyrins, a sonosensitizer in photodynamic therapy (Rosenthal et al, 2004;Jalilian et al, 2005); Gapyrazole and its derivatives, as antitumor agents for the therapy of ovarian adenocarcinoma and human lung carcinoma (Tajiri et al, 1994;Balbi et al, 2011); and Gathiolate ligands, for their dose-dependent antiproliferative effect toward cancer cells (Gallego et al, 2011). Besides low molecular weigh...…”

Novel pyrazole-5-carboxamide and pyrazole–pyrimidine derivatives: Synthesis and anticancer activity

“…It was of our interest to utilize rational chemical approaches to generate and identify novel compounds as potential telomerase inhibitors for cancer therapy. Results of structure-activity relationships (SAR) about these derivatives show that the alkyl of the position 1 or 3 should help the activity, there is some motivations provided in the design idea [17][18][19][20]. Furthermore, based on the protein TERT structure of telomerase using LigandFit module, our group has recently reported a novel docking model and we found that ASP 254 was a key residue for activity.…”

Synthesis and apoptotic activity of new pyrazole derivatives in cancer cell lines

“…Shaw et al (2010) synthesized a series of 3,5-diaryl-1H-pyrazole derivatives with apoptosis-inducing effect on OVCA cells through caspase-dependent pathways and inactivation of protein kinase B/Akt activity [14]. Balbi et al (2011) developed several pyrazole derivatives with anti-proliferative and pro-apoptotic activity through disassembly of microtubules [15].…”