2440-60-0Relevant articles and documents
CARBOCYCLIC NUCLEOSIDE ANALOGUE
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Page/Page column 11; 14, (2020/12/30)
The present invention relates to novel hydrolytically stable carbocyclic 5-aza-2-deoxycytidine and carbocyclic 5-aza-cytidine compounds and prodrugs thereof as hypomethylating agents.
Thioimidazoline based compounds reverse glucocorticoid resistance in human acute lymphoblastic leukemia xenografts
Toscan, Cara E.,Rahimi, Marwa,Bhadbhade, Mohan,Pickford, Russell,McAlpine, Shelli R.,Lock, Richard B.
, p. 6299 - 6312 (2015/06/08)
Glucocorticoids form a critical component of chemotherapy regimens for pediatric acute lymphoblastic leukemia (ALL) and the initial response to glucocorticoid therapy is a major prognostic factor, where resistance is predictive of poor outcome. A high-throughput screen identified four thioimidazoline-containing compounds that reversed dexamethasone resistance in an ALL xenograft derived from a chemoresistant pediatric ALL. The lead compound (1) was synergistic when used in combination with the glucocorticoids, dexamethasone or prednisolone. Synergy was observed in a range of dexamethasone-resistant xenografts representative of B-cell precursor ALL (BCP-ALL) and T-cell ALL. We describe here the synthesis of twenty compounds and biological evaluation of thirty two molecules that explore the structure-activity relationships (SAR) of this novel class of glucocorticoid sensitizing compounds. SAR analysis has identified that the most effective dexamethasone sensitizers contain a thioimidazoline acetamide substructure with a large hydrophobic moiety on the acetamide. This journal is
Preparation of substituted guanidine derivatives
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, (2008/06/13)
Substituted guanidine derivatives of the formula I are prepared by a) converting urea into an alkylated isourea of the formula II and b) reacting the alkylated isourea with a primary or secondary amine of the formula III where the substituents R1, R2 and R10 have the meanings explained in the description.
