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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 …
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 …
bioactive molecules. Macrocyclization is increasingly prominent in medicinal chemistry …
Macrocyclization strategy for improving candidate profiles in medicinal chemistry
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 …
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 …
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)
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 …
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
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 …
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 …
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
Overcoming resistance to third-generation tyrosine kinase inhibitors (TKIs) such as
Osimertinib, particularly due to the emergence of the C797S mutation, remains a key …
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 …
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
Sixteen new 2-substituted quinazolines were synthesized using a straightforward
methodology starting from 2-methoxybezoic acid or 3-methoxy-2-naphthoic acid. The anti …
methodology starting from 2-methoxybezoic acid or 3-methoxy-2-naphthoic acid. The anti …