89180-90-5Relevant articles and documents
2,4-DIOXO-QUINAZOLINE-6-SULFONAMIDE DERIVATIVES AS INHIBITORS OF PARG
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Paragraph 00825, (2016/07/05)
The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity wherein R1a, R1b, R1c, R1d, R1e, W, X1, X2, X3, X4, X5, X6, X7, c are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which PARG activity is implicated.
Structurally simple, potent, Plasmodium selective farnesyltransferase inhibitors that arrest the growth of malaria parasites
Glenn, Matthew P.,Chang, Sung-Youn,Hornéy, Carrie,Rivas, Kasey,Yokoyama, Kohei,Pusateri, Erin E.,Fletcher, Steven,Cummings, Christopher G.,Buckner, Frederick S.,Pendyala, Prakash R.,Chakrabarti, Debopam,Sebti, Sa?d M.,Gelb, Michael,Van Voorhis, Wesley C.,Hamilton, Andrew D.
, p. 5710 - 5727 (2007/10/03)
Third world nations require immediate access to inexpensive therapeutics to counter the high mortality inflicted by malaria. Here, we report a new class of antimalarial protein farnesyltransferase (PFT) inhibitors, designed with specific emphasis on simple molecular architecture, to facilitate easy access to therapies based on this recently validated antimalarial target. This novel series of compounds represents the first Plasmodium falciparum selective PFT inhibitors reported (up to 145-fold selectivity), with lead inhibitors displaying excellent in vitro activity (IC50 50 100 nM). Initial studies of absorption, metabolism, and oral bioavailability are reported.
Structurally simple farnesyltransferase inhibitors arrest the growth of malaria parasites
Glenn, Matthew P.,Chang, Sung-Youn,Hucke, Oliver,Verlinde, Christophe L. M. J.,Rivas, Kasey,Horney, Carrie,Yokoyama, Kohei,Buckner, Frederick S.,Pendyala, Prakash R.,Chakrabarti, Debopam,Gelb, Michael,Van Voorhis, Wesley C.,Sebti, Said M.,Hamilton, Andrew D.
, p. 4903 - 4906 (2007/10/03)
(Chemical Equation Presented) Antimalarial compounds: Structurally simple acyclic inhibitors of protein farnesyltransferase (active-site model shown) from the malaria parasite Plasmodium falciparum may allow third world countries access to an effective and inexpensive antimalarial therapy to counter the estimated half billion infections that occur annually.