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Glycogen Synthase Kinase 3 Is a Potential Drug Target for African Trypanosomiasis Therapy
TLDR
There is reasonable genetic and chemical validation of G SK-3 short as a drug target for T. brucei, and selective inhibition may be required for therapy targeting the GSK-3 enzyme, which suggests that compounds that selectively inhibit T. Brucei GSK -3 short over the human Gsk-3 enzymes can be found.
Agelastatin A: a novel inhibitor of osteopontin-mediated adhesion, invasion, and colony formation
TLDR
This study reveals, for the very first time, that (-)-agelastatin A down-regulates β-catenin expression while simultaneously up-regulating Tcf-4 and that these combined effects cause repression of OPN and inhibition of oPN-mediated malignant cell invasion, adhesion, and colony formation in vitro.
Total syntheses of the telomerase inhibitors dictyodendrin B, C, and E.
TLDR
Concise and flexible total syntheses of the pyrrolo[2,3-c]carbazole alkaloids dictyodendrin B, C, and E are described, particularly noteworthy in this context is the generation of the very labile p-quinomethide motif of dictyODendrin E.
Total synthesis of dictyodendrin B.
TLDR
It was shown that global deprotection of the peripheral -OH groups in pyrrolo[2,3-c]carbazole 13 is accompanied by spontaneous air-oxidation to form the quinone core of dictyodendrin C, a scarce marine alkaloid endowed with promising telomerase inhibitory activity.
Identification and characterization of novel small molecules as potent inhibitors of the plasmodial calcium-dependent protein kinase 1.
TLDR
A homology-based model of the kinase core domain has been built which allows rational design of the next generation of inhibitors of PfCDPK1, a calcium-dependent protein kinase expressed in Plasmodium falciparum.
New total synthesis of the marine antitumor alkaloid (-)-agelastatin A.
TLDR
A new total synthesis of (-)-agelastatin A (1) has been achieved from the chiral oxazolidinone (-)-3.5% using Hunig's base after the pyrrole nucleus was brominated.
Enantiospecific formal total synthesis of the tumor and GSK-3 beta inhibiting alkaloid, (-)-agelastatin A.
TLDR
An enantiospecific total synthesis of Weinreb's advanced intermediate 2 for (-)-agelastatin A has been achieved from the Hough-Richardson aziridine 8 with highly regioselective trans-diaxial ring-opening of 8 with azide ion to set up the vicinal diamido functionality present within (-)-2.
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