Comprehensive Survey of Chemical Libraries for Drug Discovery and Chemical Biology: 2006

Dolle, Roland E.; Bourdonnec, Bertrand Le; Goodman, Catherine; Morales, Guillermo A.; Salvino, Joseph M.; Zhang, Wei

doi:10.1021/cc700111e

Cited by 79 publications

(24 citation statements)

References 485 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Keywords: asymmetric hydrophobic tails · cationic lipids · DNA delivery · liposomes · nonviral vectors · solid-phase synthesis tic agents, [25] as well as cationic lipids. [11,12,22] The synthesized lipids were evaluated for their transfection efficiency into different cells, including human embryonic kidney cells (HEK293), colorectal adenocarcinoma (COLO 205), canine osteosarcoma (D17), human cervical adenocarcinoma (HeLa), and human prostate adenocarcinoma (PC3)…”

Section: Introductionmentioning

confidence: 99%

High Transfection Efficiency of Cationic Lipids with Asymmetric Acyl–Cholesteryl Hydrophobic Tails

Radchatawedchakoon

Krajarng

Niyomtham

et al. 2011

Chemistry A European J

View full text Add to dashboard Cite

The ability of a nonviral gene delivery system to overcome extra- and intracellular barriers is a critical issue for the future clinical applications of gene therapy. In recent years much effort has been focused on the development of a variety of DNA carriers, and cationic liposomes have become the most common nonviral gene delivery system. One hundred and eighty novel cationic lipids with asymmetric acyl-cholesteryl hydrophobic tails were synthesized by parallel solid-phase chemistry. The liposomes were prepared and gel retardation assays were used to study the binding efficiency between the prepared liposome and the DNA. Transfection efficiencies of the lipids were evaluated against various mammalian cells, such as human embryonic kidney (HEK293), human cervical adenocarcinoma (HeLa), canine osteosarcoma (D17), colorectal adenocarcinoma (COLO 205), and human prostate adenocarcinoma (PC3) cells. The lipids with an acyl portion at the terminal part of the polyamine backbone exhibited higher transfection efficiency than those with the acyl portion as an internal part of the backbone. These compounds also showed higher transfection efficiency and lower cytotoxicity than the commercially available agents, Effectene, DOTAP, and DC-Chol.

show abstract

Section: Introductionmentioning

confidence: 99%

High Transfection Efficiency of Cationic Lipids with Asymmetric Acyl–Cholesteryl Hydrophobic Tails

Radchatawedchakoon

Krajarng

Niyomtham

et al. 2011

Chemistry A European J

View full text Add to dashboard Cite

show abstract

“…Essential to this goal are two fundamental features i) the production and access to libraries of skeletally diverse small molecules and ii) biological evaluation and identification of new probes 2. Such small molecules have had a dramatic effect in recent years providing invaluable insight into biological targets and the development of therapeutic agents for curing disease 3.…”

Section: Introductionmentioning

confidence: 99%

Reagent based DOS: A “Click, Click, Cyclize” strategy to probe chemical space

2010

View full text Add to dashboard Cite

The synthesis of small organic molecules as probes for discovering new therapeutic agents has been an important aspect of chemical-biology. Herein we report a reagent-based, diversity-oriented synthetic (DOS) strategy to probe chemical and biological space via a "Click, Click, Cyclize" protocol. In this DOS approach, three sulfonamide linchpins underwent cyclization protocols with a variety of reagents to yield a collection of structurally diverse S-heterocycles. In silico analysis is utilized to evaluate the diversity of the compound collection against chemical space (PC analysis), shape space (PMI) and polar surface area (PSA) calculations.

show abstract

“…31 chains in the imidazole and pyrimidine rings led to a series of monosubstituted purine products. For preparation of disubstituted purine derivatives, appropriately substituted tosyl isocyanides were used.…”

Section: Chemistrymentioning

confidence: 99%

A convenient synthesis and molecular modeling study of novel purine and pyrimidine derivatives as CDK2/cyclin A3 inhibitors

Elgazwy

Ismail

Elzahabi³

2010

Bioorganic & Medicinal Chemistry

View full text Add to dashboard Cite

Comprehensive Survey of Chemical Libraries for Drug Discovery and Chemical Biology: 2006

Abstract: This is the thirteenth installment of the comprehensive survey series in high throughput chemistry. 1 Biologically active libraries reported in 2009 are captured in Tables 1-5 under the headings of proteases, nonproteolytic enzymes, GPCRs, nonGPCRs, and oncolytics/ antiinfectives.

Cited by 79 publications

References 485 publications

High Transfection Efficiency of Cationic Lipids with Asymmetric Acyl–Cholesteryl Hydrophobic Tails

High Transfection Efficiency of Cationic Lipids with Asymmetric Acyl–Cholesteryl Hydrophobic Tails

Reagent based DOS: A “Click, Click, Cyclize” strategy to probe chemical space

A convenient synthesis and molecular modeling study of novel purine and pyrimidine derivatives as CDK2/cyclin A3 inhibitors

Contact Info

Product

Resources

About