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Discovery and Optimization of Novel Pyrazolopyrimidines as Potent and Orally Bioavailable Allosteric HIV-1 Integrase Inhibitors.
Allosteric inhibitors of HIV-1 integrase that bind to the LEDGF/p75 interaction site and disrupt the structure of the integrase multimer that is required for the HIV- 1 maturation are described. Expand
Solid phase synthesis of novel pyrrolidinedione analogs as potent HIV-1 integrase inhibitors.
A solid-phase route was developed which facilitates the simultaneous variation at R(1, R(2), and R(3) of the pyrrolidinedione scaffold of the HIV-1 integrase inhibitor library. Expand
Nocathiacin I analogues: synthesis, in vitro and in vivo biological activity of novel semi-synthetic thiazolyl peptide antibiotics.
Several nocathiacin I analogues (4-35) were synthesized and evaluated for their antibacterial activity and retained very good in vitro and in vivo antib bacterial activity. Expand
Synthesis, in vitro, and in vivo antibacterial activity of nocathiacin I thiol-Michael adducts.
The synthesis and antibacterial activity of a series of nocathiacin I derivatives (4-20) containing polar water solubilizing groups is described. Thiol-Michael adducts containing acidic polar groupsExpand
Novel semi-synthetic nocathiacin antibiotics: synthesis and antibacterial activity of bis- and mono-O-alkylated derivatives.
The excellent in vivo activity and improved water solubility of phosphate analogues 3m and 4g suggest their use as potential pro-drugs. Expand
Synthesis and antibacterial activity of nocathiacin I analogues.
Stereoselective reduction of dehydroalanine double bond in nocathiacin I afforded the primary amide 2, which upon coupling with a variety of amines furnished amides 4-32 that have retained very good antibacterial activity and improved aqueous solubility. Expand
Profound Catalyst Effects in the Generation and Reactivity of Carbenoid-Derived Cyclic Ylides
Good yields of ylide-derived [1,2]-shift (or in some cases [1,4]-shift) products were obtained upon treatment of amino diazo ketone subtrates 3b,c and alkoxy diazo ketone subtrates 5b,c with solubleExpand
Organic reactions in frozen water: Michael addition of amines and thiols to the dehydroalanine side chain of nocathiacins
Abstract Nocathiacins are densely functionalized cyclic thiazolyl peptide natural products with potent in vitro and in vivo antibacterial activity against a variety of gram-positive bacteria,Expand
Discovery of a fluoroindolo[2,3-a]carbazole clinical candidate with broad spectrum antitumor activity in preclinical tumor models superior to the marketed oncology drug, CPT-11.
A series of fluoroglycosylated fluoroindolocarbazoles was examined with respect to their topoisomerase I activity, cytotoxicity, and selectivity. The lead clinical candidate from this series,Expand