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Synthesis and Biological Evaluation of the First Triple Inhibitors of Human Topoisomerase 1, Tyrosyl-DNA Phosphodiesterase 1 (Tdp1), and Tyrosyl-DNA Phosphodiesterase 2 (Tdp2).
Tdp1 and Tdp2 are two tyrosyl-DNA phosphodiesterases that can repair damaged DNA resulting from topoisomerase inhibitors and a variety of other DNA-damaging agents. Both Tdp1 and Tdp2 inhibitionExpand
Synthesis of indolo[4,3-bc]phenanthridine-6,11(2H,12H)-diones using the schiff base–homophthalic anhydride cyclization reaction
ABSTRACT A novel indolophenanthridine ring system has been synthesized via the Schiff base–homophthalic anhydride cyclization followed by thionyl chloride–mediated dehydrogenation and intramolecularExpand
Design and Synthesis of Chlorinated and Fluorinated 7-Azaindenoisoquinolines as Potent Cytotoxic Anticancer Agents That Inhibit Topoisomerase I.
The 7-azaindenoisoquinolines are cytotoxic topoisomerase I (Top1) inhibitors. Previously reported representatives bear a 3-nitro group. The present report documents the replacement of the potentiallyExpand
Design, Synthesis, and Biological Evaluation of Potential Prodrugs Related to the Experimental Anticancer Agent Indotecan (LMP400).
Indenoisoquinoline topoisomerase I (Top1) inhibitors are a novel class of anticancer agents with two compounds in clinical trials. Recent metabolism studies of indotecan (LMP400) led to the discoveryExpand
Novel Fluoroindenoisoquinoline Non-Camptothecin Topoisomerase I Inhibitors
Contrary to other anticancer targets, topoisomerase I (TOP1) is targeted by only one chemical class of FDA-approved drugs: topotecan and irinotecan, the derivatives of the plant alkaloid,Expand
Indenoisoquinoline Topoisomerase Inhibitors Strongly Bind and Stabilize the MYC Promoter G-Quadruplex and Downregulate MYC.
MYC is one of the most important oncogenes and is overexpressed in the majority of cancers. G-Quadruplexes are noncanonical four-stranded DNA secondary structures that have emerged as attractiveExpand
Synthesis of Thiazole, Triazole, Pyrazolo[3,4-b]-Pyridinyl-3-Phenylthiourea, Aminopyrazolo[3,4-b]Pyridine Derivatives and Their Biological Evaluation
Abstract The pyrazolopyridine derivatives 1a,b reacted with phenylisothiocyanate (2), nitrous acid and cinnamonitrile derivatives 5a,b to afford the correspondedExpand
Synthesis of Benzo[1,6]naphthyridinones Using the Catellani Reaction.
An intramolecular version of the Catellani reaction was optimized for one-step synthesis of bulky N-substituted benzo[1,6]naphthyridinones with good to excellent yields. The optimized reaction ofExpand
Design, synthesis and molecular modeling study of certain 4-Methylbenzenesulfonamides with CDK2 inhibitory activity as anticancer and radio-sensitizing agents.
Two series of 2-aminopyridine derivatives 6-17 and tyrphostin AG17 analogs 18-22 bearing 4-methylbenzenesulfonamide moiety were designed and synthesized as anticancer compounds. The synthesizedExpand
Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) Series.
The present account describes the discovery and development of a new benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) JAK inhibitory chemotype that has produced selective JAK inhibitors.Expand