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Relevant academic research and scientific papers

Design, synthesis and structure-activity relationship study of novel urea compounds as FGFR1 inhibitors to treat metastatic triple-negative breast cancer

Triple-negative breast cancer (TNBC) is an aggressive type of cancer characterized by higher metastatic and reoccurrence rates, where approximately one-third of TNBC patients suffer from the metastasis in the brain. At the same time, TNBC shows good responses to chemotherapy, a feature that fuels the search for novel compounds with therapeutic potential in this area. Recently, we have identified novel urea-based compounds with cytotoxicity against selected cell lines and with the ability to cross the blood-brain barrier in vivo. We have synthesized and analyzed a library of more than 40 compounds to elucidate the key features responsible for the observed activity. We have also identified FGFR1 as a molecular target that is affected by the presence of these compounds, confirming our data using in silico model. Overall, we envision that these compounds can be further developed for the potential treatment of metastatic breast cancer.

SUBSTITUTED BISPHENYLALKYLUREA COMPOUNDS AND METHODS OF TREATING BREAST CANCER

Disclosed is a composition and method for a therapeutic treatment that is able to combat triple negative breast cancers (TNBCs). The class of urea compounds acts by blocking at inhibiting the mTOR signaling pathway, which, as a central regulator of mammalian metabolism and physiology that when inhibited leads to the induction of autophagocytosis. The disclosed compounds are further capable of reinitiating the p53 cycle as well as inhibition of the BNIP3/BNIP3L pathway. The disclosed compounds also shows the ability to cross the blood-brain-barrier where metastases can form. This new drug has the potential to be a powerful new treatment to combat invasive TNBCs. Formula (I).

SUBSTITUTED BISPHENYLALKYLUREA COMPOUNDS AND METHODS

Disclosed is a composition and method for a therapeutic treatment that is able to combat neuroinflammation caused by diseases and disorders such as Alzheimer's disease, Parkinson's disease, and traumatic brain injury. The class of urea compounds acts by blocking at targeted receptors in the brain that contribute to the increase in inflammation. Combinations of receptors, HI receptor, H2 receptor, dopamine transporter (DAT), and/or 5HT3C receptor, are individually and/or collectively inhibited by the same compositions of the present disclosure, and this ability leads to a decrease in brain edema. The DAT inhibitory effects additionally maintains dopamine levels in a patient.

Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity

Several recent reports have highlighted the feasibility of the use of penfluridol, a well-known antipsychotic agent, as a chemotherapeutic agent. In vivo experiments have confirmed the cytotoxic activity of penfluridol in triple-negative breast cancer model, lung cancer model, and further studies have been proposed to assess its anticancer activity and viability for the treatment of glioblastomas. However, penfluridol anticancer activity was observed at a dosage significantly higher than that administered in antipsychotic therapy, thus raising the concern for the potential onset of CNS side effects in patients undergoing intensive pharmacological treatment. In this study, we evaluate the potential CNS toxicity of penfluridol side by side with a set of analogs.

Lactones, XX. - Grignardation Followed by Phase-Transfer Oxidation: A Convenient Synthesis of δ,δ-Disubstituted δ-Lactones from δ-Valerolactone

A Grignardation-oxidation sequence, without isolation of intermediates, easily transfers δ-valerolactone (4) into Δ,δ-disubstituted δ-lactones 6.The synthesis of δ,δ-diphenyl-δ-valerolactone (6a) served as an exsample for a detailed investigation of the r