Researchers from Birla Institute of Technology & Science, Pilani and Jadavpur University have reported novel HDAC3 inhibitors as potential candidates for the treatment of breast cancer. Synthesis and optimization of a series of pyrazino-hydrazide-based HDAC3 inhibitors led to the characterization of compound [I] as the lead candidate with potent HDAC3 inhibitory activity (IC50=14 nM) and at least 121-fold selectivity.
Among all human papillomavirus (HPV) types described so far, the two most abundant – HPV16 and HPV18 – are responsible for 71% of all cervical cancers. The vaccines currently used are effective in preventing viral infection, but have no effect on already infected or maligned cells.
Researchers from Umm Al-Qura University and affiliated organizations have published details on the discovery and preclinical evaluation of anticancer candidates acting both as COX-2 inhibitors and tubulin-targeting agents.
Proteomics International Pty Ltd has developed a new blood-based diagnostic test called the Promarkereso that identifies patients with esophageal adenocarcinoma as well as patients with a pre-malignant condition called Barrett’s esophagus that can arise from chronic acid reflux.
China Welfare Institute International Peace Maternity and Child Health Hospital and East China University of Science & Technology have jointly developed aza-phenothiazine derivatives reported to be useful for the treatment of endometrial cancer.
Research at RIKEN has led to the identification of furanocoumarin derivatives acting as dihydroorotate dehydrogenase (DHODH) inhibitors reported to be useful for the treatment of cancer and viral infections.
Phosphatidylinositol 3-kinase α (PI3Kα) inhibitors have been reported in a Synnovation Therapeutics Inc. patent as useful for the treatment of cancer, PIK3CA-related overgrowth spectrum, congenital lipomatous overgrowth, vascular malformations, epidermal naevi and skeletal abnormalities.
Ono Pharmaceutical Co. Ltd. has entered into a drug discovery collaboration agreement with Adimab LLC to discover and develop innovative antibody drugs in the oncology field.
Researchers from Fudan University and affiliated organizations presented the discovery of novel PIM kinase inhibitors for the treatment of acute myeloid leukemia (AML). A literature-aided molecular hybridization strategy was applied to synthesize a structurally novel compound, based on an N-pyridinyl amide scaffold. Subsequent optimization showed that the positional isomerization of pyridine N toward to Lys67 resulted in a decrease of potency while increased freedom of solvent fragment toward Asp128/Glu171 led to an increase in activity.
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