685533-72-6Relevant articles and documents
Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors
La Pietra, Valeria,Sartini, Stefania,Botta, Lorenzo,Antonelli, Alessandro,Ferrari, Silvia Martina,Fallahi, Poupak,Moriconi, Alessio,Coviello, Vito,Quattrini, Luca,Ke, Yi-Yu,Hsing-Pang, Hsieh,Da Settimo, Federico,Novellino, Ettore,La Motta, Concettina,Marinelli, Luciana
supporting information, p. 491 - 505 (2018/03/21)
It is now known that “gain of function” mutations of RET (REarranged during Transfection) kinase are specific and key oncogenic events in the onset of thyroid gland cancers such as the Medullary Thyroid Carcinoma (MTC). Although a number of RET inhibitors exist and are capable of inhibiting RET variants, in which mutations are outside the enzyme active site, the majority becomes dramatically ineffective when mutations are within the protein active site (V804L and V804M). Pursuing a receptor-based virtual screening against the kinase domain of RET, we found that compound 5 is able to inhibit efficiently both wild type and V804L mutant RET. Compound 5 was able to significantly reduce proliferation of both commercially available TT cell lines and surgical thyroid tissues obtained from patients with MTC and displayed a suitable drug-like profile, thus standing out as a promising candidate for further development towards the treatment of clinically unresponsive MTC.
ANTIBACTERIAL COMPOUNDS AND METHODS OF USING SAME
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Page/Page column 15, (2010/11/03)
Embodiments of the present invention provide novel antibacterials that target penicillin-binding proteins or other important cellular targets. Methods for inhibiting growth (reproduction, etc.) of bacteria using compounds described herein are also provided. Various embodiments exhibit activity against gram positive bacteria, such as certain strains of Entercoccus and Staphylococcus aureus.
ANTIBACTERIAL COMPOUNDS AND METHODS OF USING SAME
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Page/Page column 36-37, (2009/05/29)
Embodiments of the present invention provide novel antibactehals that target penicillin-binding proteins or other important cellular targets. Methods for inhibiting growth (reproduction, etc.) of bacteria using compounds described herein are also provided. Various embodiments exhibit activity against gram positive bacteria, such as certain strains of Entercoccus and Staphylococcus aureus.
METHYLENE UREA DERIVATIVES
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Page 296, (2008/06/13)
The present invention relates to methylene urea derivatives of formula (I), the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.
