Songwen Lin
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View article: Correction: Hou et al. S-72, a Novel Orally Available Tubulin Inhibitor, Overcomes Paclitaxel Resistance via Inactivation of the STING Pathway in Breast Cancer. Pharmaceuticals 2023, 16, 749
Correction: Hou et al. S-72, a Novel Orally Available Tubulin Inhibitor, Overcomes Paclitaxel Resistance via Inactivation of the STING Pathway in Breast Cancer. Pharmaceuticals 2023, 16, 749 Open
In the original publication [...]
View article: Targeting DDX3X suppresses progression of KRAS-driven lung cancer by disrupting antioxidative homeostasis and inducing ferroptosis
Targeting DDX3X suppresses progression of KRAS-driven lung cancer by disrupting antioxidative homeostasis and inducing ferroptosis Open
Approximately 30% of human cancers carry various RAS mutations, including KRAS , NRAS , and HRAS . Among these mutations, KRAS is the most prevalent isoform detected in lung cancer. While several small molecular inhibitors targeting specif…
View article: Design, Synthesis, and Bioevaluation of Novel Reversibly Photoswitchable PI3K Inhibitors Based on Phenylazopyridine Derivatives toward Light-Controlled Cancer Treatment
Design, Synthesis, and Bioevaluation of Novel Reversibly Photoswitchable PI3K Inhibitors Based on Phenylazopyridine Derivatives toward Light-Controlled Cancer Treatment Open
Photopharmacology is an emerging approach for achieving light-controlled drug activity. Herein, we design and synthesize a novel series of photoswitchable PI3K inhibitors by replacing a sulfonamide moiety with an azo group in a 4-methylqui…
View article: Design, synthesis and biological evaluation of a novel PSMA–PI3K small molecule drug conjugate
Design, synthesis and biological evaluation of a novel PSMA–PI3K small molecule drug conjugate Open
A novel PSMA–PI3K small molecule drug conjugate has been prepared, highlighting its potential in targeted cancer therapy.
View article: Discovery of Novel Photoswitchable Pd-L1 Inhibitors Toward Precision Cancer Immunotherapy
Discovery of Novel Photoswitchable Pd-L1 Inhibitors Toward Precision Cancer Immunotherapy Open
View article: Rational design and optimization of novel 4-methyl quinazoline derivatives as PI3K/HDAC dual inhibitors with benzamide as zinc binding moiety for the treatment of acute myeloid leukemia
Rational design and optimization of novel 4-methyl quinazoline derivatives as PI3K/HDAC dual inhibitors with benzamide as zinc binding moiety for the treatment of acute myeloid leukemia Open
View article: Discovery of a Novel Photocaged PI3K Inhibitor Capable of Real-Time Reporting of Drug Release
Discovery of a Novel Photocaged PI3K Inhibitor Capable of Real-Time Reporting of Drug Release Open
A novel photocaged PI3K inhibitor 2 was designed and synthesized by introducing a cascade photocaging group to block its key interaction with the kinase. Upon UV light irradiation, the photocaged compound released a highly potent PI…
View article: S-72, a Novel Orally Available Tubulin Inhibitor, Overcomes Paclitaxel Resistance via Inactivation of the STING Pathway in Breast Cancer
S-72, a Novel Orally Available Tubulin Inhibitor, Overcomes Paclitaxel Resistance via Inactivation of the STING Pathway in Breast Cancer Open
Microtubule-targeting agents are widely used as active anticancer drugs. However, drug resistance always emerges after their long-term use, especially in the case of paclitaxel, which is the cornerstone of all subtypes of breast cancer tre…
View article: Rational Design and Optimization of Novel 4-Methyl Quinazoline Derivatives as Pi3k/Hdac Dual Inhibitors with Benzamide as Zinc Binding Moiety for the Treatment of Acute Myeloid Leukemia
Rational Design and Optimization of Novel 4-Methyl Quinazoline Derivatives as Pi3k/Hdac Dual Inhibitors with Benzamide as Zinc Binding Moiety for the Treatment of Acute Myeloid Leukemia Open
View article: Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site
Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site Open
Targeting the colchicine binding site on tubulin is a promising strategy to develop cancer therapeutics. Herein, we describe our systematic structure-activity relationship studies of benzamide derivatives that lead to an identification of …
View article: Discovery of a novel photoswitchable PI3K inhibitor toward optically-controlled anticancer activity
Discovery of a novel photoswitchable PI3K inhibitor toward optically-controlled anticancer activity Open
View article: Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma
Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma Open
View article: Design and Optimization of Thienopyrimidine Derivatives as Potent and Selective PI3Kδ Inhibitors for the Treatment of B-Cell Malignancies
Design and Optimization of Thienopyrimidine Derivatives as Potent and Selective PI3Kδ Inhibitors for the Treatment of B-Cell Malignancies Open
Phosphoinositide 3-kinase δ (PI3Kδ) plays a critical role in B lymphocyte (B-cell) development and activation and has been a validated target for the treatment of B-cell malignancies. Herein, we report a series of thienopyrimidine derivati…
View article: The PI3K Inhibitor XH30 Enhances Response to Temozolomide in Drug-Resistant Glioblastoma via the Noncanonical Hedgehog Signaling Pathway
The PI3K Inhibitor XH30 Enhances Response to Temozolomide in Drug-Resistant Glioblastoma via the Noncanonical Hedgehog Signaling Pathway Open
Glioblastoma multiforme (GBM) is the most common malignant tumor of the central nervous system. Temozolomide (TMZ)–based adjuvant treatment has improved overall survival, but clinical outcomes remain poor; TMZ resistance is one of the main…
View article: A novel PI3K inhibitor XH30 suppresses orthotopic glioblastoma and brain metastasis in mice models
A novel PI3K inhibitor XH30 suppresses orthotopic glioblastoma and brain metastasis in mice models Open
Glioblastoma is carcinogenesis of glial cells in central nervous system and has the highest incidence among primary brain tumors. Brain metastasis, such as breast cancer and lung cancer, also leads to high mortality. The available medicine…
View article: Design, Synthesis, and Biological Evaluation of a Novel Photocaged PI3K Inhibitor toward Precise Cancer Treatment
Design, Synthesis, and Biological Evaluation of a Novel Photocaged PI3K Inhibitor toward Precise Cancer Treatment Open
Aberrant activation of the PI3K pathway has been intensively targeted for cancer therapeutics for decades, leading to more than 40 PI3K inhibitors advanced into clinical trials. However, it is increasingly noticed that PI3K inhibitors ofte…
View article: Discovery of new thieno[2,3-d]pyrimidine and thiazolo[5,4-d]pyrimidine derivatives as orally active phosphoinositide 3-kinase inhibitors
Discovery of new thieno[2,3-d]pyrimidine and thiazolo[5,4-d]pyrimidine derivatives as orally active phosphoinositide 3-kinase inhibitors Open
View article: Identification of Novel Thiazolo[5,4-b]Pyridine Derivatives as Potent Phosphoinositide 3-Kinase Inhibitors
Identification of Novel Thiazolo[5,4-b]Pyridine Derivatives as Potent Phosphoinositide 3-Kinase Inhibitors Open
A series of novel 2-pyridyl, 4-morpholinyl substituted thiazolo[5,4-b]pyridine analogues have been designed and synthesized in this paper. These thiazolo[5,4-b]pyridines were efficiently prepared in seven steps from commercially available …
View article: Discovery of 4-Methylquinazoline Based PI3K Inhibitors for the Potential Treatment of Idiopathic Pulmonary Fibrosis
Discovery of 4-Methylquinazoline Based PI3K Inhibitors for the Potential Treatment of Idiopathic Pulmonary Fibrosis Open
Idiopathic pulmonary fibrosis (IPF) is a progressive and fatal lung disease, and its molecular pathogenesis remains poorly understood. Recently, emerging evidence demonstrates that the PI3K signaling transduction pathway is linked to the p…
View article: Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases Open
Polypharmacology is a promising paradigm in modern drug discovery. Herein, we have discovered a series of novel PI3K and HDAC dual inhibitors in which the hydroxamic acid moiety as the zinc binding functional group was introduced to a quin…
View article: Switching the site-selectivity of C–H activation in aryl sulfonamides containing strongly coordinating N-heterocycles
Switching the site-selectivity of C–H activation in aryl sulfonamides containing strongly coordinating N-heterocycles Open
Switching the site-selectivity of C–H activation in aryl sulfonamides containing strongly coordinating N-heterocycles was achieved using a RhIII-catalyst.
View article: Discovery and Optimization of 2-Amino-4-methylquinazoline Derivatives as Highly Potent Phosphatidylinositol 3-Kinase Inhibitors for Cancer Treatment
Discovery and Optimization of 2-Amino-4-methylquinazoline Derivatives as Highly Potent Phosphatidylinositol 3-Kinase Inhibitors for Cancer Treatment Open
Increased phosphatidylinositol 3-kinase (PI3K) signaling is among the most common alterations in cancer, spurring intensive efforts to develop new cancer therapeutics that target this pathway. In this work, we discovered a series of novel …
View article: Bt354 as a new STAT3 signaling pathway inhibitor against triple negative breast cancer
Bt354 as a new STAT3 signaling pathway inhibitor against triple negative breast cancer Open
Inhibition of the signal transducer and activator of transcription 3 (STAT3) signalling pathway has been considered as a novel therapeutic strategy to treat human cancers with constitutively active STAT3. In this study, we screened 1563 co…
View article: Discovery of new thienopyrimidine derivatives as potent and orally efficacious phosphoinositide 3-kinase inhibitors
Discovery of new thienopyrimidine derivatives as potent and orally efficacious phosphoinositide 3-kinase inhibitors Open
View article: Design, synthesis and anti-tumor activities of cyclic phosphoramidate mustard-quinazoline conjugates
Design, synthesis and anti-tumor activities of cyclic phosphoramidate mustard-quinazoline conjugates Open
View article: Design, synthesis and biological evaluation of quinazoline–phosphoramidate mustard conjugates as anticancer drugs
Design, synthesis and biological evaluation of quinazoline–phosphoramidate mustard conjugates as anticancer drugs Open
View article: Discovery of a Novel Series of Thienopyrimidine as Highly Potent and Selective PI3K Inhibitors
Discovery of a Novel Series of Thienopyrimidine as Highly Potent and Selective PI3K Inhibitors Open
Inhibition of the phosphoinositide 3-kinase (PI3K)/AKT/mammalian target of rapamycin (mTOR) signaling pathway provides a promising new approach for cancer therapy. Through a rational design, a novel series of thienopyrimidine was discovere…