Rational multitargeted drug design strategy from the perspective of a medicinal chemist

X Li, X Li, F Liu, S Li, D Shi - Journal of Medicinal Chemistry, 2021 - ACS Publications
The development of multitarget-directed ligands (MTDLs) has become a widely focused
research topic, but rational design remains as an enormous challenge. This paper reviews …

Hybrid drugs—a strategy for overcoming anticancer drug resistance?

M Szumilak, A Wiktorowska-Owczarek, A Stanczak - Molecules, 2021 - mdpi.com
Despite enormous progress in the treatment of many malignancies, the development of
cancer resistance is still an important reason for cancer chemotherapy failure. Increasing …

Designing multi-targeted agents: An emerging anticancer drug discovery paradigm

R Fu, Y Sun, W Sheng, D Liao - European journal of medicinal chemistry, 2017 - Elsevier
The dominant paradigm in drug discovery is to design ligands with maximum selectivity to
act on individual drug targets. With the target-based approach, many new chemical entities …

Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors

AKA Bass, MS El-Zoghbi, ESM Nageeb… - European journal of …, 2021 - Elsevier
Despite the encouraging clinical progress of chemotherapeutic agents in cancer treatment,
innovation and development of new effective anticancer candidates still represents a …

Kinase and histone deacetylase hybrid inhibitors for cancer therapy

Y Luan, J Li, JA Bernatchez, R Li - Journal of medicinal chemistry, 2018 - ACS Publications
Histone deacetylases (HDACs), encompassing at least 18 members, are promising targets
for anticancer drug discovery and development. To date, five histone deacetylase inhibitors …

[HTML][HTML] CUDC-907 in relapsed/refractory diffuse large B-cell lymphoma, including patients with MYC-alterations: results from an expanded phase I trial

Y Oki, KR Kelly, I Flinn, MR Patel, R Gharavi, A Ma… - …, 2017 - ncbi.nlm.nih.gov
CUDC-907 is a first-in-class, oral small molecule inhibitor of both HDAC (class I and II) and
PI3K (class Iα, β, and δ) enzymes, with demonstrated anti-tumor activity in multiple pre …

MYC the oncogene from hell: Novel opportunities for cancer therapy

A Papadimitropoulou, M Makri, G Zoidis - European Journal of Medicinal …, 2024 - Elsevier
Cancer comprises a heterogeneous disease, characterized by diverse features such as
constitutive expression of oncogenes and/or downregulation of tumor suppressor genes …

Targeting phosphoinositide 3-kinase (PI3K) in head and neck squamous cell carcinoma (HNSCC)

K Jung, H Kang, R Mehra - Cancers of the head & neck, 2018 - Springer
The landscape of head and neck squamous cell carcinoma (HNSCC) has been changing
rapidly due to growing proportion of HPV-related disease and development of new …

Dual HDAC and PI3K inhibition abrogates NFκB-and FOXM1-mediated DNA damage response to radiosensitize pediatric high-grade gliomas

S Pal, D Kozono, X Yang, W Fendler, W Fitts, J Ni… - Cancer research, 2018 - AACR
Aberrant chromatin remodeling and activation of the PI3K pathway have been identified as
important mediators of pediatric high-grade glioma (pHGG) and diffuse intrinsic pontine …

MYC drives platinum resistant SCLC that is overcome by the dual PI3K-HDAC inhibitor fimepinostat

J Chen, AC Guanizo, WSN Jakasekara… - Journal of Experimental …, 2023 - Springer
Background Small cell lung cancer (SCLC) is an aggressive neuroendocrine cancer with an
appalling overall survival of less than 5%(Zimmerman et al. J Thor Oncol 14: 768-83, 2019) …