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Quinazolinone-Based Anticancer Agents: Synthesis, Antiproliferative SAR, Antitubulin Activity, and Tubulin Co-crystal Structure.
Quinazolinone-based anticancer agents were designed, decorated with functional groups from a 2-methoxyestradiol-based microtubule disruptor series, incorporating the aryl sulfamate motif of steroidExpand
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Steroidomimetic Tetrahydroisoquinolines for the Design of New Microtubule Disruptors
Structure–activity relationship translation offers an expeditious means for discovery of new active series. This approach was applied to discover tetrahydroisoquinoline (THIQ)-based steroidomimeticExpand
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Tetrahydroisoquinolinone‐Based Steroidomimetic and Chimeric Microtubule Disruptors
A structure–activity relationship (SAR) translation strategy was used for the discovery of tetrahydroisoquinoline (THIQ)‐based steroidomimetic and chimeric microtubule disruptors based upon aExpand
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Synthesis of polyfunctional indoles and related heterocycles mediated by cesium and potassium bases
A general preparation of 2-substituted indoles starting from functionalized 2-alkynylanilines has been developed. This base mediated reaction has also been used to synthesize the heterocyclic core ofExpand
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Synthesis, antitubulin, and antiproliferative SAR of analogues of 2-methoxyestradiol-3,17-O,O-bis-sulfamate.
The synthesis and antiproliferative activity of analogues of estradiol 3,17-O,O-bis-sulfamates (E2bisMATEs) are discussed. Modifications of the C-17 substituent reveal that an H-bond acceptor isExpand
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Preparation and Reactions of Functionalized Arylmagnesium Reagents
Functionalized magnesium reagents have been prepared via an iodine-magnesium exchange. These reagents can be either trapped directly with aldehydes or transmetallated to copper or zinc to participateExpand
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Structure-activity relationships of C-17-substituted estratriene-3-O-sulfamates as anticancer agents.
The synthesis and antiproliferative activities of analogues of 2-substituted estradiol-3,17-O,O-bis-sulfamates (E2bisMATEs) are discussed. Modifications of the C-17 substituent confirm that an H-bondExpand
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Synthesis, Antitubulin, and Antiproliferative SAR of C3/C1‐Substituted Tetrahydroisoquinolines
The syntheses and antiproliferative activities of novel substituted tetrahydroisoquinoline derivatives and their sulfamates are discussed. Biasing of conformational populations through substitutionExpand
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