[HTML][HTML] Small molecules, inhibitors of DNA-PK, targeting DNA repair, and beyond

D Davidson, L Amrein, L Panasci… - Frontiers in pharmacology, 2013 - frontiersin.org
Many current chemotherapies function by damaging genomic DNA in rapidly dividing cells
ultimately leading to cell death. This therapeutic approach differentially targets cancer cells …

Medicinal chemistry of oxazines as promising agents in drug discovery

DS Zinad, A Mahal, RK Mohapatra… - Chemical biology & …, 2020 - Wiley Online Library
Oxazines have brought much synthetic interest due to their extensive biological activities.
These are the important category of heterocycles, which may be formally derived from …

Phosphatidylinositol 3-kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring

M Andrs, J Korabecny, D Jun, Z Hodny… - Journal of medicinal …, 2015 - ACS Publications
Phosphatidylinositol 3-kinases (PI3Ks) and phosphatidylinositol 3-kinase-related protein
kinases (PIKKs) are two related families of kinases that play key roles in regulation of cell …

Design, synthesis of benzimidazole tethered 3, 4-dihydro-2H-benzo [e][1, 3] oxazines as anticancer agents

S Gali, D Raghu, V Mallikanti, V Thumma… - Molecular Diversity, 2024 - Springer
Abstract A series of novel 3-(1H-benzo [d] imidazol-2-yl)-3, 4-dihydro-2H-benzo [e][1, 3]
oxazine analogues synthesized through a two-step synthetic protocol. The structure of the …

Rational design, synthesis, pharmacophore modeling, and docking studies for identification of novel potent DNA-PK inhibitors

S Ihmaid, HEA Ahmed, AAS Ali, YE Sherif… - Bioorganic …, 2017 - Elsevier
Drugs of cancer based upon ionizing radiation or chemotherapeutic treatment may affect
breaking of DNA double strand in cell. DNA-PK enzyme has emerged as an attractive target …

Synthesis, structure elucidation, DNA-PK and PI3K and anti-cancer activity of 8-and 6-aryl-substituted-1-3-benzoxazines

R Morrison, JMA Al-Rawi, IG Jennings… - European journal of …, 2016 - Elsevier
Abstract The synthesis of 6-aryl, 8-aryl, and 8-aryl-6-chloro-2-morpholino-1, 3-benzoxazines
with potent activity against PI3K and DNA-PK is described. Synthesis of thirty one analogues …

Identification of 6-Anilino Imidazo[4,5-c]pyridin-2-ones as Selective DNA-Dependent Protein Kinase Inhibitors and Their Application as Radiosensitizers

CR Hong, LP Liew, WW Wong… - Journal of Medicinal …, 2024 - ACS Publications
The dominant role of non-homologous end-joining in the repair of radiation-induced double-
strand breaks identifies DNA-dependent protein kinase (DNA-PK) as an excellent target for …

Synthesis, DNA-PK inhibition, anti-platelet activity studies of 2-(N-substituted-3-aminopyridine)-substituted-1, 3-benzoxazines and DNA-PK and PI3K inhibition …

SK Ihmaid, JMA Al-Rawi, CJ Bradley… - European journal of …, 2012 - Elsevier
A number of new 2-(pyridin-3-ylamino)-4H-(substituted) benz [e]-1, 3-oxazin-4-ones were
synthesized 10a–g. These were then reacted with the hydro-halogen salt of 2, 3 and 4-(halo …

Design, synthesis, docking studies and biological screening of 2-pyrimidinyl-2, 3-dihydro-1H-naphtho [1, 2-e][1, 3] oxazines as potent tubulin polymerization …

R Gawali, R Bhosale, N Nagesh… - Journal of …, 2023 - Taylor & Francis
A series of novel substituted 2-pyrimidinyl-2, 3-dihydro-1 H-naphtho [1, 2-e][1, 3] oxazine
analogs have been designed and synthesized based on structure-activity relationships from …

An Inverse Electron Demand Azo-Diels–Alder Reaction of o-Quinone Methides and Imino Ethers: Synthesis of Benzocondensed 1,3-Oxazines

DV Osipov, VA Osyanin, GD Khaysanova… - The Journal of …, 2018 - ACS Publications
We have studied the reactions of o-quinone methide precursors with imino ethers. The
reaction provides a versatile route to substituted 1, 3-benzoxazines. The proposed reaction …