The DOI matches its Crossref record; 39 of the 39 references it cites were found in a registry or an index.
4-[3-(4-Cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2 H-phthalazin-1-one: A Novel Bioavailable Inhibitor of Poly(ADP-ribose) Polymerase-1
Open accessAbstract
Poly(ADP-ribose) polymerase activation is an immediate cellular response to metabolic-, chemical-, or ionizing radiation-induced DNA damage and represents a new target for cancer therapy. In this article, we disclose a novel series of substituted 4-benzyl-2 H-phthalazin-1-ones that possess high inhibitory enzyme and cellular potency for both PARP-1 and PARP-2. Optimized compounds from the series also demonstrate good pharmacokinetic profiles, oral bioavailability, and activity in vivo in an SW620 colorectal cancer xenograft model. 4-[3-(4-Cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2 H-phthalazin-1-one (KU-0059436, AZD2281) 47 is a single digit nanomolar inhibitor of both PARP-1 and PARP-2 that shows standalone activity against BRCA1-deficient breast cancer cell lines. Compound 47 is currently undergoing clinical development for the treatment of BRCA1- and BRCA2-defective cancers.
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Self-citationSpecific killing of BRCA2-deficient tumours with inhibitors of poly(ADP-ribose) polymerase
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The Therapeutic Potential of Poly(ADP-Ribose) Polymerase Inhibitors
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Self-citation(ADP-ribose)n participates in DNA excision repair
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Cited by
Inhibition of Poly(ADP-Ribose) Polymerase in Tumors from BRCA Mutation Carriers
Fong, P. C., Boss, D. S., Yap, T. A., Tutt, A., Wu, P., Mergui-Roelvink, M., Mortimer, P., Swaisland, H., Lau, A., O'Connor, M. J., et al. (2009) · New England Journal of Medicine · doi:10.1056/nejmoa0900212 · Cited by 3,634
Self-citationPARP inhibition: PARP1 and beyond
Rouleau, M., Patel, A., Hendzel, M. J., Kaufmann, S. H., & Poirier, G. G. (2010) · Nature Reviews Cancer · doi:10.1038/nrc2812 · Cited by 1,298
Mouchiroud, L., Houtkooper, R. H., Moullan, N., Katsyuba, E., Ryu, D., Cantó, C., Mottis, A., Jo, Y.-S., Viswanathan, M., Schoonjans, K., et al. (2013) · Cell · doi:10.1016/j.cell.2013.06.016 · Cited by 1,210
State-of-the-art strategies for targeting the DNA damage response in cancer
Pilié, P. G., Tang, C., Mills, G. B., & Yap, T. A. (2019) · Nature Reviews Clinical Oncology · doi:10.1038/s41571-018-0114-z · Cited by 1,189
Gelmon, K. A., Tischkowitz, M., Mackay, H., Swenerton, K., Robidoux, A., Tonkin, K., Hirte, H., Huntsman, D., Clemons, M., Gilks, B., et al. (2011) · The Lancet Oncology · doi:10.1016/s1470-2045(11)70214-5 · Cited by 1,117
Metadata
- Authors
- Menear, K. A., Adcock, C., Boulter, R., Cockcroft, X.-L., Copsey, L., Cranston, A., Dillon, K. J., Drzewiecki, J., Garman, S., Gomez, S., Javaid, H., Kerrigan, F., Knights, C., Lau, A., Loh, V. M., Matthews, I. T. W., Moore, S., O’Connor, M. J., Smith, G. C. M., & Martin, N. M. B.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2008-09-19
- Volume
- 51
- Issue
- 20
- Pages
- 6581-6591
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2014035904
- Cited by
- 584
- References
- 39
- FWCI
- 10.63
- Type
- journal article
- Language
- en
- Open access
- green
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- CoChat. (2026). Citation check: 4-[3-(4-Cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2 H-phthalazin-1-one: A Novel Bioavailable Inhibitor of Poly(ADP-ribose) Polymerase-1. https://app.cochat.ai/papers/10.1021/jm8001263
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- Menear, K. A., Adcock, C., Boulter, R., Cockcroft, X.-L., Copsey, L., Cranston, A., Dillon, K. J., Drzewiecki, J., Garman, S., Gomez, S., Javaid, H., Kerrigan, F., Knights, C., Lau, A., Loh, V. M., Matthews, I. T. W., Moore, S., O’Connor, M. J., Smith, G. C. M., & Martin, N. M. B. (2008). 4-[3-(4-Cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2 H-phthalazin-1-one: A Novel Bioavailable Inhibitor of Poly(ADP-ribose) Polymerase-1. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm8001263
Data sources
Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
