Quinolines, a perpetual, multipurpose scaffold in medicinal chemistry

P Yadav, K Shah - Bioorganic Chemistry, 2021 - Elsevier
Quinoline is a versatile pharmacophore, a privileged scaffold and an outstanding fused
heterocyclic compound with a wide range of pharmacological prospective such as …

The design and discovery of topoisomerase I inhibitors as anticancer therapies

E Martín-Encinas, A Selas, F Palacios… - Expert Opinion on Drug …, 2022 - Taylor & Francis
Introduction Cancer has been identified as one of the leading causes of death worldwide.
The biological target of some anticancer agents is topoisomerase I, an enzyme involved in …

Asymmetric Auto‐Tandem Palladium Catalysis for 2, 4‐Dienyl Carbonates: Ligand‐Controlled Divergent Synthesis

JX Zhu, ZC Chen, W Du… - Angewandte Chemie …, 2022 - Wiley Online Library
Developing new asymmetric auto‐tandem catalysis processes, especially in a divergent
manner, is highly attractive but extremely challenging. Presented herein is a palladium …

Intermolecular diastereoselective annulation of azaarenes into fused N-heterocycles by Ru (II) reductive catalysis

H Zhao, Y Wu, C Ci, Z Tan, J Yang, H Jiang… - Nature …, 2022 - nature.com
Derivatization of azaarenes can create molecules of biological importance, but reductive
functionalization of weakly reactive azaarenes remains a challenge. Here the authors show …

Aza-Povarov Reaction. A Method for the Synthesis of Fused Tetracyclic Chromeno[4,3-d]pyrido[1,2-a]pyrimidines

E Martín-Encinas, L Lopez-Aguileta… - The Journal of …, 2024 - ACS Publications
A cornerstone in drug discovery is the development of strategies to provide privileged small
molecules with specific structural and stereochemical complexity, allowing access to new …

A patent review of topoisomerase I inhibitors (2016–present)

A Selas, E Martin-Encinas, M Fuertes… - Expert Opinion on …, 2021 - Taylor & Francis
Introduction Topoisomerases are important targets for therapeutic improvement in the
treatment of some diseases, including cancer. Inhibitors and poisons of topoisomerase I can …

A multicomponent protocol for the synthesis of highly functionalized γ-lactam derivatives and their applications as antiproliferative agents

X Del Corte, A López-Francés, A Maestro… - Pharmaceuticals, 2021 - mdpi.com
An efficient synthetic methodology for the preparation of 3-amino 1, 5-dihydro-2 H-pyrrol-2-
ones through a multicomponent reaction of amines, aldehydes, and pyruvate derivatives is …

Fused chromeno and quinolino [1, 8] naphthyridines: Synthesis and biological evaluation as topoisomerase I inhibitors and antiproliferative agents

E Martin-Encinas, G Rubiales, BR Knudsen… - Bioorganic & Medicinal …, 2021 - Elsevier
Abstract The synthesis of 1, 8-naphthyridine derivatives fused with other heterocycles, such
as chromenes and quinolines, as well as their behaviour as topoisomerase I inhibitors is …

Sc(OTf)3-Mediated [4 + 2] Annulations of N-Carbonyl Aryldiazenes with Cyclopentadiene to Construct Cinnoline Derivatives: Azo-Povarov Reaction

X Jiménez-Aberásturi, F Palacios… - The Journal of Organic …, 2022 - ACS Publications
We disclose the first accomplishment of the azo-Povarov reaction involving Sc (OTf) 3-
catalyzed [4+ 2] annulations of N-carbonyl aryldiazenes with cyclopentadiene in chloroform …

Electro-organic synthesis of C-5 sulfenylated amino uracils: optimization and exploring topoisomerase-I based anti-cancer profile

P Rani, S Chahal, R Kumar, P Kumar, A Negi… - Bioorganic …, 2023 - Elsevier
Cancer is spreading worldwide and is one of the leading causes of death. The use of
existing chemotherapeutic agents is frequently limited due to side effects. As a result, it is …