Discover Community Create You

Loading publication...

Noodle always counts identifier-free feature events for service operation. With your permission, Google Analytics can also estimate audience and engagement. Search text, publication identifiers, cookies, IP addresses and browser fingerprints are never included in Noodle's first-party event counters.

Privacy details

Article

Benzothiophene-based, orally active PIK3CA H1047R mutant-selective inhibitors for the treatment of HR+/HER2- breast cancer.

European journal of medicinal chemistry - 5 Aug 2026

Zhao Sheng, Fan Xing, Jia Xiangyu, Xu Hang, Xia Yuanfeng, Lu Biao, Yang Fanglong, Wang Siqin, Jin Lei

Abstract excerpt

PI3Kα plays a key role in a variety of cellular processes, and its gene mutations are closely related to the occurrence and development of many types of cancer. Although two orthosteric PI3Kα inhibitors including Alpelisib and Inavolisib have been launched onto market, they often cause toxic and side effects due to insufficient selectivity for PIK3CA mutant protein. The development of allosteric PI3Kα inhibitors...

Read the complete abstract on PubMed

Topics

Share this publication in a Topic to start or enrich a Post.

Share to Administration, Oral
Share to Class I Phosphatidylinositol 3-Kinases

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Drug Screening Assays, Antitumor

Share to Erb-b2 Receptor Tyrosine Kinases

Share to Molecular Structure

Share to Phosphoinositide-3 Kinase Inhibitors

Share to Structure-Activity Relationship

Share to Thiophenes

Source

Identifiers

PMID: 42024964
DOI: 10.1016/j.ejmech.2026.118879

Genes

PIK3CA

Variants

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

Benzothiophene-based, orally active PIK3CA H1047R mutant-selective inhibitors for the treatment of HR+/HER2- breast cancer.PMID 42024964Read ↗

Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein.Semantic proximity Read ↗

Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα.Semantic proximity Read ↗

Difuran-substituted quinoxalines as a novel class of PI3Kα H1047R mutant inhibitors: Synthesis, biological evaluation and structure-activity relationship.Semantic proximity Read ↗

High-throughput screening campaigns against a PI3Kα isoform bearing the H1047R mutation identified potential inhibitors with novel scaffolds.Semantic proximity Read ↗

The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of ( <i>S</i> )-2-((2-(1-Isopropyl-1 <i>H</i> -1,2,4-triazol-5-yl)-5,6-dihydrobenzo[ <i>f</i> ]imidazo[1,2- <i>d</i> ][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326)Semantic proximity Read ↗

Inavolisib: a second-generation PI3Kα inhibitor in HR+/HER2-negative breast cancer.Semantic proximity Read ↗

Structural Insights into the Development of Inhibitors Against Cancer-Specific Mutations of PI3Kα.Semantic proximity Read ↗

Benzothiophenone Derivatives Targeting Mutant Forms of Estrogen Receptor-α in Hormone-Resistant Breast Cancers.Semantic proximity Read ↗

Inavolisib-based Combination Therapy for the Treatment of PIK3CAMutated HR+/HER2- Breast Cancer: An Overview.Semantic proximity Read ↗

Rational Design of Potent and Orally Efficacious PI3Kα/δ Degrader for PIK3CA Mutant Breast Cancer without Hyperglycemic Liability.Semantic proximity Read ↗

Selective covalent-allosteric tools to dissect Akt2Semantic proximity Read ↗

Discovery of novel pyrazolo[3,4-b]pyridine scaffold-based derivatives as potential PIM-1 kinase inhibitors in breast cancer MCF-7 cellsSemantic proximity Read ↗

⌁Select a neighboring publication to make it the new centre.