Novel Class of Fluorinated Pyrazolo[1,5‐a]pyrimidines as CDK5 and Bcl2 Inhibitors: Design, Synthesis, Biological Evaluation, Molecular Docking and ADME Studies

M Said Mohamed, Z Atwa Saad… - …, 2023 - Wiley Online Library
Abstract New pyrazolo [1, 5‐a] pyrimidines were designed and synthesized based on the
structural analysis of known CDK5 inhibitors. Biological evaluations showed that the IC50 of …

Development of pyrazolo [3, 4-d] pyrimidin-4-one scaffold as novel CDK2 inhibitors: Design, synthesis, and biological evaluation

F Xie, L Zhou, C Ge, X Song, H Yan - Bioorganic & Medicinal Chemistry …, 2022 - Elsevier
Abstract A series of pyrazolo [3, 4-d] pyrimidin-4-one scaffold were designed and
synthesized as novel CDK2 inhibitors. By analyzing the common motifs of various known …

Discovery of new pyrazolopyridine, furopyridine, and pyridine derivatives as CDK2 inhibitors: Design, synthesis, docking studies, and anti-proliferative activity

AAH Abdel-Rahman, AKF Shaban, IF Nassar… - Molecules, 2021 - mdpi.com
New pyridine, pyrazoloyridine, and furopyridine derivatives substituted with naphthyl and
thienyl moieties were designed and synthesized starting from 6-(naphthalen-2-yl)-2-oxo-4 …

Design, Synthesis, In Vitro, and In Silico Studies of New N5-Substituted-pyrazolo[3,4-d]pyrimidinone Derivatives as Anticancer CDK2 Inhibitors

WA Zaki, SM El-Sayed, M Alswah, A El-Morsy… - Pharmaceuticals, 2023 - mdpi.com
CDK2 is a key player in cell cycle processes. It has a crucial role in the progression of
various cancers. Hepatocellular carcinoma (HCC) and colorectal cancer (CRC) are two …

Discovery of pyrazolo [3, 4-d] pyrimidine and pyrazolo [4, 3-e][1, 2, 4] triazolo [1, 5-c] pyrimidine derivatives as novel CDK2 inhibitors: synthesis, biological and …

IF Nassar, MTA Aal, WA El-Sayed, MAE Shahin… - RSC …, 2022 - pubs.rsc.org
CDK2 inhibition is an appealing target for cancer treatment that targets tumor cells in a
selective manner. A new set of small molecules featuring the privileged pyrazolo [3, 4-d] …

Mechanistic selectivity investigation and 2D-QSAR study of some new antiproliferative pyrazoles and pyrazolopyridines as potential CDK2 inhibitors

GS Hassan, HH Georgey, EZ Mohammed… - European Journal of …, 2021 - Elsevier
Novel series of diphenyl-1H-pyrazoles (4a-g) and pyrazolo [3, 4-b] pyridines (5a-g and 7a-i)
were synthesized and evaluated for their antiproliferative activity against breast cancer cell …

Identification of 3-(piperazinylmethyl)benzofuran derivatives as novel type II CDK2 inhibitors: design, synthesis, biological evaluation, and in silico insights

WM Eldehna, RM Maklad, H Almahli… - Journal of Enzyme …, 2022 - Taylor & Francis
In the current work, a hybridisation strategy was adopted between the privileged building
blocks, benzofuran and piperazine, with the aim of designing novel CDK2 type II inhibitors …

Novel pyrazolo [3, 4-d] pyrimidines as potential cytotoxic agents: Design, synthesis, molecular docking and CDK2 inhibition

M Maher, AE Kassab, AF Zaher… - Anti-Cancer Agents in …, 2019 - ingentaconnect.com
Background: Pyrazolo [3, 4-d] pyrimidine scaffold was reported to possess potent cytotoxic
and CDK2 inhibitory activity as analogue of roscovitine. Objective: To design and synthesize …

Exploring new quinazolin‐4(3H)‐one derivatives as CDK2 inhibitors: Design, synthesis, and anticancer evaluation

BT Ibrahim, HA Allam, NM El‐Dydamony… - Drug Development …, 2024 - Wiley Online Library
In the present work, five series of new 2, 3‐disubstituted quinazolin‐4 (3H)‐ones 4a–c, 5a–
d, 6a–g, 7a, b, and 9a–c were designed, synthesized, and screened in vitro for their cytotoxic …

Design, synthesis and biological evaluation of methylenehydrazine-1-carboxamide derivatives with (5-((4-(pyridin-3-yl) pyrimidin-2-yl) amino)-1H-indole scaffold …

H Hu, J Wu, M Ao, X Zhou, B Li, Z Cui, T Wu, L Wang… - Bioorganic …, 2020 - Elsevier
In continuation of our previous work on the investigation of CDK9 inhibitors bearing indole
moiety for the discovery of novel anticancer agents, novel methylenehydrazine-1 …