A series of 6-aminocarbonyl pyrrolo[2,1-f][1,2,4]triazine derivatives were designed by scaffold hopping strategy. The IC values of compound 14a against PI3Ks were measured, showing selective activity against p110α and p110δ with ICs of 122 nM and 119 nM respectively. All the synthesized compounds were evaluated for their antiproliferative activity against human cancer cells by SRB assay. Compounds 14a, 14p and 14q exhibited potent antiproliferative activity against five types of human cancer cells and the PK property of 14q was also investigated here.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2020.127194 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Flavonoids and Kavalactones Isolated from Seeds of Alpinia katsumadai Hayata. and Their Cytotoxic Activities.
Chem Biodivers
January 2025
Guizhou Medical University, School of Pharmaceutical Sciences, University Town, Gui'an New District, 550025, Guiyang, CHINA.
An unrevealed dihydroflavone-monoterpene conjugate (1), two unrevealed kavalactones (2-3, including one with an uncommon side chain), and thirteen previously identified compounds (4-16) were extracted from Alpinia katsumadai Hayata. seeds. The two-dimension structures of the new compounds were authenticated utilizing HRESIMS as well as NMR spectral analysis, while their absolute chiral configurations were ascertained either by correlating the experimental and simulated values of electronic circular dichroism (ECD) patterns or conducting X-ray diffraction experiments.
View Article and Find Full Text PDFDiscovery of a potent PROTAC degrader for RNA demethylase FTO as antileukemic therapy.
Acta Pharm Sin B
December 2024
School of Pharmaceutical Science and Technology, Hangzhou Institute for Advanced Study, University of Chinese Academy of Sciences, Hangzhou 310024, China.
The fat mass and obesity-associated protein (FTO) is an RNA demethylase required for catalytic demethylation of -methyladenosine (mA); it is highly expressed and functions as an oncogene in acute myeloid leukemia (AML). Currently, the overarching objective of targeting FTO is to precisely inhibit the catalytic activity. Meanwhile, whether FTO degradation also exerts antileukemic effects remains unknown.
View Article and Find Full Text PDFPyrazoline Derivatives: Exploring the Synthesis and Development of New Ligands for Anti-Cancer Therapy.
Med Chem
January 2025
School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, India.
Pyrazoline is a 5-membered ring that has two adjacent nitrogen. It has gained advanced attention from medical and organic chemists due to very low cytotoxic activities. It is applicable and more applied in research fields and has various pharmacological activities, including cardiovascular, anti-tumor, and anti-cancer properties.
View Article and Find Full Text PDFERα dysfunction caused by ESR1 mutations and therapeutic pressure promotes lineage plasticity in ER breast cancer.
Nat Cancer
January 2025
Department of Discovery Oncology, Genentech, South San Francisco, CA, USA.
Multiple next-generation molecules targeting estrogen receptor α (ERα) are being investigated in breast cancer clinical trials, encompassing thousands of women globally. Development of these molecules was partly motivated by the discovery of resistance-associated mutations in ESR1 (encodes ERα). Here, we studied the impact of ERα antagonist/degraders against Esr1 mutations expressed in mouse mammary glands.
View Article and Find Full Text PDF[Chemical constituents from stems and leaves of Mycetia hainanensis and their anti-rheumatoid arthritis activities].
Zhongguo Zhong Yao Za Zhi
December 2024
Engineering Research Center for Industrialization of Southern Medicinal Plants Resources of Hainan Province, Hainan Normal University Haikou 571158, China Key Laboratory of Southern Medicinal Plants Resources of Haikou City, Hainan Normal University Haikou 571158, China Key Laboratory of Tropical Medicinal Resource Chemistry of Ministry of Education, Hainan Normal University Haikou 571158, China.
The chemical constituents from the stems and leaves of Mycetia hainanensis were isolated by silica gel, ODS gel, and Sephadex LH-20 gel column chromatography and preparative HPLC. The chemical structures of all the isolated compounds were identified on the basis of their physicochemical properties, spectroscopic data, as well as the comparison of their physicochemical and spectroscopic data with the reported data in literature. Twelve compounds were isolated from the 85% ethanol extract of the stems and leaves of M.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!