PROTACs: great opportunities for academia and industry
X Sun, H Gao, Y Yang, M He, Y Wu, Y Song… - Signal transduction and …, 2019 - nature.com
Although many kinds of therapies are applied in the clinic, drug-resistance is a major and
unavoidable problem. Another disturbing statistic is the limited number of drug targets, which …
unavoidable problem. Another disturbing statistic is the limited number of drug targets, which …
PI3K inhibitors: review and new strategies
M Zhang, H Jang, R Nussinov - Chemical science, 2020 - pubs.rsc.org
The search is on for effective specific inhibitors for PI3Kα mutants. PI3Kα, a critical lipid
kinase, has two subunits, catalytic and inhibitory. PIK3CA, the gene that encodes the p110α …
kinase, has two subunits, catalytic and inhibitory. PIK3CA, the gene that encodes the p110α …
Discovery of 2-{3-[2-(1-Isopropyl-3-methyl-1H-1,2–4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC …
CO Ndubaku, TP Heffron, ST Staben… - Journal of medicinal …, 2013 - ACS Publications
Dysfunctional signaling through the phosphoinositide 3-kinase (PI3K)/AKT/mTOR pathway
leads to uncontrolled tumor proliferation. In the course of the discovery of novel benzoxepin …
leads to uncontrolled tumor proliferation. In the course of the discovery of novel benzoxepin …
How many kinases are druggable? A review of our current understanding
There are over 500 human kinases ranging from very well-studied to almost completely
ignored. Kinases are tractable and implicated in many diseases, making them ideal targets …
ignored. Kinases are tractable and implicated in many diseases, making them ideal targets …
Phthalimide conjugations for the degradation of oncogenic PI3K
W Li, C Gao, L Zhao, Z Yuan, Y Chen… - European journal of …, 2018 - Elsevier
Abstract PI3K/Akt/mTOR pathway is crucial for carcinogenesis and its inhibitors have made a
great progress in cancer treatment. However, there is still a great developing space for PI3K …
great progress in cancer treatment. However, there is still a great developing space for PI3K …
Structural determinants of isoform selectivity in PI3K inhibitors
Phosphatidylinositol 3-kinases (PI3Ks) are important therapeutic targets for the treatment of
cancer, thrombosis, and inflammatory and immune diseases. The four highly homologous …
cancer, thrombosis, and inflammatory and immune diseases. The four highly homologous …
Phosphoinositide 3-kinase (PI3K) inhibitors and breast cancer: an overview of current achievements
A Bertucci, F Bertucci, A Gonçalves - Cancers, 2023 - mdpi.com
Simple Summary Breast cancer remains the fourth-leading cause of death worldwide, and
therapeutic improvement is warranted. The phosphatidylinositol 3-kinase (PI3K) pathway is …
therapeutic improvement is warranted. The phosphatidylinositol 3-kinase (PI3K) pathway is …
Palladium-catalyzed annulative allylic alkylation for regioselective construction of indole-fused medium-sized cyclic ethers
LQ Chen, CF Zhu, S Zhang, BY Liu, SJ Tu… - Chinese Chemical …, 2023 - Elsevier
A new palladium-catalyzed annulative allylic alkylation (AAA) reaction of 2-(indol-2-yl)
phenols with dual allylic electrophiles such as isobutylene dicarbonate and butene …
phenols with dual allylic electrophiles such as isobutylene dicarbonate and butene …
Recent developments regarding the use of thieno [2, 3-d] pyrimidin-4-one derivatives in medicinal chemistry, with a focus on their synthesis and anticancer properties
K Bozorov, JY Zhao, B Elmuradov, A Pataer… - European Journal of …, 2015 - Elsevier
It is generally understood that the antitumor properties of synthetic heterocyclic compounds
are among the most powerful properties that can be made use in medicinal chemistry. More …
are among the most powerful properties that can be made use in medicinal chemistry. More …
A facile method for preparation and evaluation of the antimicrobial efficiency of various heterocycles containing thieno[2,3-d]pyrimidine
Heterocyclic compounds play an important role in the field of pharmaceutical chemistry,
especially compounds containing hybrid bioactive moieties. So in continuation of our work …
especially compounds containing hybrid bioactive moieties. So in continuation of our work …