Macrocycles and macrocyclization in anticancer drug discovery: Important pieces of the puzzle

C Zhang, F Liu, Y Zhang, C Song - European Journal of Medicinal …, 2024‏ - Elsevier
Increasing disease-related proteins have been identified as novel therapeutic targets.
Macrocycles are emerging as potential solutions, bridging the gap between conventional …

The Missing Link (er): A Roadmap to Macrocyclization in Drug Discovery

C Brudy, C Walz, M Spiske, JK Dreizler… - Journal of medicinal …, 2024‏ - ACS Publications
Macrocycles are one of nature's preferred choices to generate large but cell-permeable
bioactive molecules. Macrocyclization is increasingly prominent in medicinal chemistry …

Macrocyclization strategy for improving candidate profiles in medicinal chemistry

O Darlami, R Pun, SH Ahn, SH Kim, D Shin - European journal of medicinal …, 2024‏ - Elsevier
Macrocycles are defined as cyclic compounds with 12 or more members. In medicinal
chemistry, they are categorized based on their core chemistry into cyclic peptides and …

Discovery of selective and potent macrocyclic CDK9 inhibitors for the treatment of osimertinib-resistant non-small-cell lung cancer

T Wu, B Yu, Y Xu, Z Du, Z Zhang, Y Wang… - Journal of Medicinal …, 2023‏ - ACS Publications
Effectiveness of epidermal growth factor receptor (EGFR) inhibitors, including Osimertinib,
for treating non-small-cell lung cancer (NSCLC) is limited due to the continuous emergence …

Structure–activity relationship studies based on quinazoline derivatives as EGFR kinase inhibitors (2017–present)

A Șandor, I Ionuț, G Marc, I Oniga, D Eniu, O Oniga - Pharmaceuticals, 2023‏ - mdpi.com
The epidermal growth factor receptor (EGFR) plays a critical role in the tumorigenesis of
various forms of cancer. Targeting the mutant forms of EGFR has been identified as an …

Synthesis of pyrazole-based macrocycles leads to a highly selective inhibitor for MST3

JA Amrhein, LM Berger, DI Balourdas… - Journal of Medicinal …, 2023‏ - ACS Publications
MST1, MST2, MST3, MST4, and YSK1 are conserved members of the mammalian sterile 20-
like serine/threonine (MST) family that regulate cellular functions such as proliferation and …

A patent review of selective CDK9 inhibitors in treating cancer

T Wu, X Wu, Y Xu, R Chen, J Wang, Z Li… - Expert Opinion on …, 2023‏ - Taylor & Francis
Introduction The dysregulation of CDK9 protein is greatly related to the proliferation and
differentiation of various cancers due to its key role in the regulation of RNA transcription …

Catalytic Lysine745 targeting strategy in fourth-generation EGFR tyrosine kinase inhibitors to address C797S mutation resistance

BR Patil, HM Patel - European Journal of Medicinal Chemistry, 2025‏ - Elsevier
Overcoming resistance to third-generation tyrosine kinase inhibitors (TKIs) such as
Osimertinib, particularly due to the emergence of the C797S mutation, remains a key …

Multi-omics strategy reveals that Cordyceps sinensis ameliorates sepsis-associated acute kidney injury via reprogramming of mitochondrial energy metabolism and …

L Chen, T Yang, J Wu, G Cheng, M Zhao… - Acta Materia …, 2024‏ - scienceopen.com
Cordyceps sinensis (CS) has been widely used as a dietary supplement or traditional
medicine for the prevention, treatment, and prognostication of various diseases, because of …

[HTML][HTML] Synthesis and Biological Evaluation of 2-Substituted Quinazolin-4(3H)-Ones with Antiproliferative Activities

M Karelou, D Kampasis, AD Kalampaliki, L Persoons… - Molecules, 2023‏ - mdpi.com
Sixteen new 2-substituted quinazolines were synthesized using a straightforward
methodology starting from 2-methoxybezoic acid or 3-methoxy-2-naphthoic acid. The anti …