Selective PARP1 inhibitors, PARP1-based dual-target inhibitors, PROTAC PARP1 degraders, and prodrugs of PARP1 inhibitors for cancer therapy

X Peng, W Pan, F Jiang, W Chen, Z Qi, W Peng… - Pharmacological …, 2022 - Elsevier
Poly ADP-ribose polymerase (PARP) plays a critical role in many cellular processes such as
DNA damage repair, gene transcription and cell apoptosis. Therefore, targeting PARP …

Contribution of Knoevenagel condensation products toward the development of anticancer agents: An updated review

R Tokala, D Bora, N Shankaraiah - ChemMedChem, 2022 - Wiley Online Library
Knoevenagel condensation is an entrenched, prevailing, prominent arsenal following
greener principles in the generation of α, β‐unsaturated ketones/carboxylic acids by …

Small molecule tractable PARP inhibitors: Scaffold construction approaches, mechanistic insights and structure activity relationship

A Thakur, M Rana, J Mathew, S Nepali, CH Pan… - Bioorganic …, 2023 - Elsevier
Diverse drug design strategies viz. molecular hybridization, substituent installation, scaffold
hopping, isosteric replacement, high-throughput screening, induction and separation of …

Design and synthesis of some new 6-bromo-2-(pyridin-3-yl)-4-substituted quinazolines as multi tyrosine kinase inhibitors

AK Farouk, HA Allam, E Rashwan, RF George… - Bioorganic …, 2022 - Elsevier
The present study involves design and synthesis of five series of 6-bromo-2-(pyridin-3-yl)-4-
substituted quinazolines 9a-l, 11a-e, 13a-c, 14a-f and 15a-e. Candidates 9a-l and 11a-e …

Aqueous C–H aminomethylation of phenols by iodine catalysis

ZH Zhou, B Wang, Y Ding, TP Loh… - Chemical …, 2023 - pubs.rsc.org
A transition-metal-free strategy regarding an iodine–sodium percarbonate catalysis to
achieve the ortho-aminomethylation of phenols in aqueous media has been developed. This …

[HTML][HTML] TsOH-catalyzed dehydroxylative cross-coupling of alcohols with phenols: rapid access to propofol derivatives

Y Liang, C Liu, Y Li, L Ouyang - RSC advances, 2024 - pubs.rsc.org
Modification of the parent structure of molecules often alters their physicochemical
properties and biological activities. Herein, a practical, efficient, and highly regioselective C …

Cr-Catalyzed Direct ortho-Aminomethylation of Phenols

J Shi, Y Wang, Q Bu, B Liu, B Dai… - The Journal of Organic …, 2021 - ACS Publications
We developed a Cr-catalyzed strategy for the regioselective formation of Csp2–Csp3 bonds
through the direct and efficient ortho-aminomethylation of N, N-dimethylanilines with …

Design, Synthesis and Activity Evaluation of New Phthalazinone PARP Inhibitors

M Huang, J Ren, Y Wang, X Chen, J Yang… - Chemical and …, 2021 - jstage.jst.go.jp
Abstract Poly (ADP-ribose) polymerase (PARP) is a significant therapeutic target for the
treatment of numerous human diseases. Olaparib has been approved as a PARP inhibitor …

Discovery of highly potent PARP7 inhibitors for cancer immunotherapy

J Yang, B Liu, W Yan, X Zhao, C Wang, Q Zhu… - Bioorganic …, 2024 - Elsevier
PARP7 has been proven to play an important role in immunity. Substantial upregulation of
PARP7 is observed in numerous cancerous cell types, consequently resulting in the …

Design, synthesis, and biological activity of guaiazulene derivatives

Z Ma, X Han, J Ren, K Liu, W Zhang… - Chemistry & …, 2023 - Wiley Online Library
Guaiazulene and related derivatives were famous for diverse biological activities. In an effort
to discover new highly efficient candidate drugs derived from guaiazulene, four series of …