[HTML][HTML] The use of spirocyclic scaffolds in drug discovery

Y Zheng, CM Tice, SB Singh - Bioorganic & Medicinal Chemistry Letters, 2014 - Elsevier
Owing to their inherent three-dimensionality and structural novelty, spiro scaffolds have
been increasingly utilized in drug discovery. In this brief review, we highlight selected …

Drugging the p53 pathway: understanding the route to clinical efficacy

KH Khoo, CS Verma, DP Lane - Nature reviews Drug discovery, 2014 - nature.com
The tumour suppressor p53 is the most frequently mutated gene in human cancer, with more
than half of all human tumours carrying mutations in this particular gene. Intense efforts to …

Small-molecule inhibitors of the MDM2–p53 protein–protein interaction (MDM2 Inhibitors) in clinical trials for cancer treatment: miniperspective

Y Zhao, A Aguilar, D Bernard… - Journal of medicinal …, 2015 - ACS Publications
Design of small-molecule inhibitors (MDM2 inhibitors) to block the MDM2–p53 protein–
protein interaction has been pursued as a new cancer therapeutic strategy. In recent years …

Catalytic enantioselective construction of sulfur-containing tetrasubstituted carbon stereocenters

JS Yu, HM Huang, PG Ding, XS Hu, F Zhou… - ACS Catalysis, 2016 - ACS Publications
Sulfur-containing tetrasubstituted carbon stereocenters are widely present in natural
products, drugs, and biologically active compounds. Catalytic enantioselective construction …

Discovery of Novel Spiro[3H-indole-3,2′-pyrrolidin]-2(1H)-one Compounds as Chemically Stable and Orally Active Inhibitors of the MDM2–p53 Interaction

A Gollner, D Rudolph, H Arnhof, M Bauer… - Journal of medicinal …, 2016 - ACS Publications
Scaffold modification based on Wang's pioneering MDM2–p53 inhibitors led to novel,
chemically stable spiro-oxindole compounds bearing a spiro [3 H-indole-3, 2′-pyrrolidin]-2 …

Discovery and Optimization of Indoline-Based Compounds as Dual 5-LOX/sEH Inhibitors: In Vitro and In Vivo Anti-Inflammatory Characterization

I Cerqua, S Musella, LK Peltner, D D'Avino… - Journal of Medicinal …, 2022 - ACS Publications
The design of multitarget drugs represents a promising strategy in medicinal chemistry and
seems particularly suitable for the discovery of anti-inflammatory drugs. Here, we describe …

Chronic inflammation and cancer: potential chemoprevention through nuclear factor kappa B and p53 mutual antagonism

S Pal, A Bhattacharjee, A Ali, NC Mandal… - Journal of …, 2014 - Springer
Activation of nuclear factor-kappa B (NF-κ B) as a mechanism of host defense against
infection and stress is the central mediator of inflammatory responses. A normal (acute) …

Chiral Binaphthyl‐Based Iodonium Salt (Hypervalent Iodine (III)) as Hydrogen‐and Halogen‐Bonding Bifunctional Catalyst: Insight into Abnormal Counteranion Effect …

Y Yoshida, T Fujimura, T Mino… - Advanced Synthesis & …, 2022 - Wiley Online Library
Asymmetric construction of chiral N, S‐acetal skeletons is important because they are widely
present in natural products and pharmaceuticals. Halogen‐bonding is a unique interaction …

Spiro-oxindoles as a promising class of small molecule inhibitors of p53–MDM2 interaction useful in targeted cancer therapy

AK Gupta, M Bharadwaj, A Kumar… - Topics in Current …, 2017 - Springer
As a result of the toxicity of currently available anticancer drugs and the inefficiency of
chemotherapeutic treatments, the design and discovery of effective and selective antitumor …

Organocatalytic asymmetric synthesis of spiro-oxindole piperidine derivatives that reduce cancer cell proliferation by inhibiting MDM2–p53 interaction

MC Yang, C Peng, H Huang, L Yang, XH He… - Organic …, 2017 - ACS Publications
Asymmetric synthesis of pharmacologically interesting piperidine-fused spiro-oxindole
derivatives has been achieved via an organocatalytic Michael/aza-Henry/hemiaminalization …