A5027849320- DNA Repair Mechanisms
- Cancer therapeutics and mechanisms
- PARP inhibition in cancer therapy
- Synthesis and Biological Evaluation
- Integrated Circuits and Semiconductor Failure Analysis
- Chemical Synthesis and Analysis
- Asthma and respiratory diseases
- Mast cells and histamine
- Receptor Mechanisms and Signaling
- Ubiquitin and proteasome pathways
- Histone Deacetylase Inhibitors Research
- Protein Degradation and Inhibitors
University of Sussex
2025
Novartis (Switzerland)
2015
Thermo Fisher Scientific (United Kingdom)
2008
GW Pharmaceuticals (United Kingdom)
2008
Poly(ADP-ribose) polymerase activation is an immediate cellular response to metabolic-, chemical-, or ionizing radiation-induced DNA damage and represents a new target for cancer therapy. In this article, we disclose novel series of substituted 4-benzyl-2 H-phthalazin-1-ones that possess high inhibitory enzyme potency both PARP-1 PARP-2. Optimized compounds from the also demonstrate good pharmacokinetic profiles, oral bioavailability, activity in vivo SW620 colorectal xenograft model....
Copper catalyzed aldehyde–alkyne–amine (A3) couplings lead to multifunctional, racemic, propargylic amines, many on a multigram scale. As part of an industrial collaboration, selection linkers was purified by chiral HPLC afford single enantiomers, the absolute configuration which determined vibrational circular dichroism (vCD). To show medicinal chemistry applications, selected were further derivatized into potential cellular probes and (+)-JQ1 containing PROTACs (proteolysis targeting...
The duocarmycins are potent antitumor agents with potential for use in the development of antibody-drug conjugates (ADCs) as well being clinical candidates their own right. In this article, we describe synthesis a duocarmycin monomer (DSA) that is suitably protected utilization solid-phase synthesis. was performed on large scale, and resulting racemic Fmoc-DSA subunit separated by supercritical fluid chromatography (SFC) into single enantiomers; its application to methodology gave series...