ArticleBioorganic chemistry2018
3H-pyrazolo[4,3-f]quinoline haspin kinase inhibitors and anticancer properties.
Article in Bioorganic chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
18 citing papers in PubMed, 41 citations in OpenAlex.
- Synthesis of 1Molecules (Basel, Switzerland) · 2025Article
- The multifaceted role of KIF15 in cancer progression and therapy.Investigational new drugs · 2025Review
- Boronic Acid-Containing 3Pharmaceuticals (Basel, Switzerland) · 2024Article
- A ComprehensiveJournal of medicinal chemistry · 2024Article
- Dual FLT3/haspin kinase inhibitor based on 3RSC medicinal chemistry · 2023Article
- Recent Advances in the Development of Pyrazole Derivatives as Anticancer Agents.International journal of molecular sciences · 2023Review
- STING antagonists, synthesizedRSC medicinal chemistry · 2023Article
- Re-sensitization of Multidrug-Resistant and Colistin-Resistant Gram-Negative Bacteria to Colistin by Povarov/Doebner-Derived Compounds.ACS infectious diseases · 2023Article
- Inhibitory Effect of the HASPIN Inhibitor CHR-6494 on BxPC-3-Luc, A Luciferase-Expressing Pancreatic Cancer Cell Line.Cell journal · 2022Article
- Induction of Paraptotic Cell Death in Breast Cancer Cells by a Novel Pyrazolo[3,4-Antioxidants (Basel, Switzerland) · 2022Article
- Facile synthesis andHeliyon · 2021Article
- Tailored Quinolines Demonstrate Flexibility to Exert Antitumor Effects through Varied Mechanisms-A Medicinal Perspective.Anti-cancer agents in medicinal chemistry · 2021Review
- Design of new disubstituted imidazo[1,2-Journal of enzyme inhibition and medicinal chemistry · 2020Article
- HASPIN kinase inhibitor CHR-6494 suppresses intestinal polyp development, cachexia, and hypogonadism in Apcmin/+ mice.European journal of cancer prevention : the official journal of the European Cancer Prevention Organisation (ECP) · 2020Article
- HSD1787, a Tetrahydro-3ACS omega · 2020Article
- Knockdown of GSG2 inhibits prostate cancer progression in vitro and in vivo.International journal of oncology · 2020Article
- GSG2 (Haspin) promotes development and progression of bladder cancer through targeting KIF15 (Kinase-12).Aging · 2020Article
- Novel Anthraquinone Compounds Inhibit Colon Cancer Cell Proliferation via the Reactive Oxygen Species/JNK Pathway.Molecules (Basel, Switzerland) · 2020Article
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
Abstract
Histone modification, a post-translational modification of histones and involving various covalent tags, such as methyl, phosphate and acetate groups, affects gene expression and hence modulates various cellular events, including growth and proliferation. Consequently histone-modifying proteins have become targets for the development of anticancer agents. Thus far, compounds that inhibit the methylation or acetylation of histones have advanced in the clinic, but inhibitors of histone phosphorylation have lagged behind. Haspin is a kinase that phosphorylates histone H3 and is a promising anticancer target. Thus far only a handful of haspin inhibitors have been reported. Using a one-flask Doebner/Povarov reaction, we synthesized a library of compounds that potently inhibit haspin with IC50 values as low as 14 nM. Some of these compounds also inhibited the proliferation of cancer cell lines HCT116, HeLa and A375. The ease of synthesis of the new haspin inhibitors, coupled with their anticancer activities make these compounds interesting leads to develop into therapeutics.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.