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Articles 1 - 5 of 5
Full-Text Articles in Physical Sciences and Mathematics
Synthesis Of An Ortho-Triazacyclophane: N,N',N''-Trimethyltribenzo-1,4,7-Triazacyclononatriene, Andria M. Panagopoulos, Matthias Zeller, Daniel P. Becker
Synthesis Of An Ortho-Triazacyclophane: N,N',N''-Trimethyltribenzo-1,4,7-Triazacyclononatriene, Andria M. Panagopoulos, Matthias Zeller, Daniel P. Becker
Chemistry: Faculty Publications and Other Works
N,N',N''-Trimethyltribenzo-1,4,7-triazacyclononatriene has been synthesized via sequential palladium-catalyzed Buchwald-Hartwig N-arylation reactions affording the 9-membered triaza o-cyclophane in 35% overall yield. An X-ray crystal structure shows the new cyclophane to have a C(2)-symmetric saddle conformation, as compared to the crown conformation exhibited by the related carbocyclic cyclotriveratrylene (CTV).
Orally Active Mmp-1 Sparing Α-Tetrahydropyranyl And Α-Piperidinyl Sulfone Matrix Metalloproteinase (Mmp) Inhibitors With Efficacy In Cancer, Arthritis, And Cardiovascular Disease, Daniel P. Becker, Thomas E. Barta, Louis J. Bedell, Terri L. Boehm
Orally Active Mmp-1 Sparing Α-Tetrahydropyranyl And Α-Piperidinyl Sulfone Matrix Metalloproteinase (Mmp) Inhibitors With Efficacy In Cancer, Arthritis, And Cardiovascular Disease, Daniel P. Becker, Thomas E. Barta, Louis J. Bedell, Terri L. Boehm
Chemistry: Faculty Publications and Other Works
α-Sulfone-α-piperidine and α-tetrahydropyranyl hydroxamates were explored that are potent inhibitors of MMP’s-2, -9, and -13 that spare MMP-1, with oral efficacy in inhibiting tumor growth in mice and left-ventricular hypertrophy in rats and in the bovine cartilage degradation ex vivo explant system. α-Piperidine 19v (SC-78080/SD-2590) was selected for development toward the initial indication of cancer, while α-piperidine and α-tetrahydropyranyl hydroxamates 19w (SC-77964) and 9i (SC-77774), respectively, were identified as backup compounds.
Palladium(Ii)-Catalyzed Dicarboxymethylation Of Chiral Allylic Alcohols: Chirality Transfer Affording Optically Active Diesters Containing Three Contiguous Chiral Centers, Othman Hamed, Patrick M. Henry, Daniel P. Becker
Palladium(Ii)-Catalyzed Dicarboxymethylation Of Chiral Allylic Alcohols: Chirality Transfer Affording Optically Active Diesters Containing Three Contiguous Chiral Centers, Othman Hamed, Patrick M. Henry, Daniel P. Becker
Chemistry: Faculty Publications and Other Works
This manuscript describes the extension of Stille’s palladium-catalyzed olefin dicarbonylation reaction to chiral allylic alcohols with chirality transfer to afford the corresponding chiral alcohol functionalized with bis-carbomethoxy esters, containing three contiguous chiral centers, in good to excellent diastereoselectivities (78–98%).
Mmp-13 Selective Isonipecotamide Alpha-Sulfone Hydroxamates, Stephen A. Kolodziej, Susan L. Hockerman, Gary A. Decrescenzo, Joseph J. Mcdonald, Grace E. Munie, Theresa R. Fletcher, Nathan Stehle, Craig Swearingen, Daniel Becker
Mmp-13 Selective Isonipecotamide Alpha-Sulfone Hydroxamates, Stephen A. Kolodziej, Susan L. Hockerman, Gary A. Decrescenzo, Joseph J. Mcdonald, Grace E. Munie, Theresa R. Fletcher, Nathan Stehle, Craig Swearingen, Daniel Becker
Chemistry: Faculty Publications and Other Works
A series of N-aryl isonipecotamide α-sulfone hydroxamate derivatives has been prepared utilizing a combination of solution-phase and resin-bound library technologies to afford compounds that are potent and highly selective for MMP-13.
Orally Bioavailable Dual Mmp-1/Mmp-14 Sparing, Mmp-13 Selective Alpha-Sulfone Hydroxamates, Daniel Becker, Stephen A. Kolodziej, Susan L. Hockerman, Terri L. Boehm, Jeffery N. Carroll
Orally Bioavailable Dual Mmp-1/Mmp-14 Sparing, Mmp-13 Selective Alpha-Sulfone Hydroxamates, Daniel Becker, Stephen A. Kolodziej, Susan L. Hockerman, Terri L. Boehm, Jeffery N. Carroll
Chemistry: Faculty Publications and Other Works
A series of phenyl piperidine α-sulfone hydroxamate derivatives has been prepared utilizing a combination of solution-phase and resin-bound library technologies to afford compounds that are potent and highly selective for MMP-13, are dual-sparing of MMP-1 and MMP-14 (MT1-MMP) and exhibit oral bioavailability in rats.