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Synthetic and medicinal chemistry of phthalazines: Recent developments, opportunities and challenges.
Zaib S, Khan I. Zaib S, et al. Bioorg Chem. 2020 Dec;105:104425. doi: 10.1016/j.bioorg.2020.104425. Epub 2020 Oct 24. Bioorg Chem. 2020. PMID: 33157344 Review.
Fused diaza-heterocycles constitute the core structure of numerous bioactive natural products and effective therapeutic drugs. Among them, phthalazines have been recognized as remarkable structural leads in medicinal chemistry due to their wide application in …
Fused diaza-heterocycles constitute the core structure of numerous bioactive natural products and effective therapeutic drugs. Among them, …
Androgen receptor inhibitor-induced "BRCAness" and PARP inhibition are synthetically lethal for castration-resistant prostate cancer.
Li L, Karanika S, Yang G, Wang J, Park S, Broom BM, Manyam GC, Wu W, Luo Y, Basourakos S, Song JH, Gallick GE, Karantanos T, Korentzelos D, Azad AK, Kim J, Corn PG, Aparicio AM, Logothetis CJ, Troncoso P, Heffernan T, Toniatti C, Lee HS, Lee JS, Zuo X, Chang W, Yin J, Thompson TC. Li L, et al. Sci Signal. 2017 May 23;10(480):eaam7479. doi: 10.1126/scisignal.aam7479. Sci Signal. 2017. PMID: 28536297 Free PMC article.
This functional state and therapeutic sensitivity is referred to as "BRCAness" and is most commonly associated with some breast cancer types. Pharmaceutical induction of BRCAness could expand the use of PARP inhibitors to other tumor types. ...
This functional state and therapeutic sensitivity is referred to as "BRCAness" and is most commonly associated with some breast cancer types …
Recent advances in the synthesis of phthalazin-1(2H)-one core as a relevant pharmacophore in medicinal chemistry.
Terán C, Besada P, Vila N, Costas-Lago MC. Terán C, et al. Eur J Med Chem. 2019 Jan 1;161:468-478. doi: 10.1016/j.ejmech.2018.10.047. Epub 2018 Oct 25. Eur J Med Chem. 2019. PMID: 30388463 Review.
Phthalazin-1(2H)-one is a diazaheterobicycle found in a wide variety of synthetic molecules relevant to several branches of chemistry, including medicinal chemistry. The versatility of phthalazinone core in drug discovery has promoted the search
Phthalazin-1(2H)-one is a diazaheterobicycle found in a wide variety of synthetic molecules relevant to several branches of
Recent synthetic strategies for the functionalization of fused bicyclic heteroaromatics using organo-Li, -Mg and -Zn reagents.
Dhayalan V, Dodke VS, Pradeep Kumar M, Korkmaz HS, Hoffmann-Röder A, Amaladass P, Dandela R, Dhanusuraman R, Knochel P. Dhayalan V, et al. Chem Soc Rev. 2024 Nov 12;53(22):11045-11099. doi: 10.1039/d4cs00369a. Chem Soc Rev. 2024. PMID: 39311874 Review.
These methods are now widely employed in organic synthetic chemistry and have proven to be particularly valuable for drug development programs in the pharmaceutical industry. ...In addition, the use of some transition metal-catalyzed processes occasionally al …
These methods are now widely employed in organic synthetic chemistry and have proven to be particularly valuable for drug deve …
Benzodiazines: recent synthetic advances.
Mathew T, Papp AÁ, Paknia F, Fustero S, Surya Prakash GK. Mathew T, et al. Chem Soc Rev. 2017 May 22;46(10):3060-3094. doi: 10.1039/c7cs00082k. Chem Soc Rev. 2017. PMID: 28452390 Review.
Benzodiazines (diazonaphthalenes with both nitrogens in the same ring) - cinnolines (1,2-benzodiazine), quinazolines (1,3-benzodiazine), phthalazines (2,3-benzodiazine) and quinoxalines (1,4-benzodiazine) - are important class of compounds with broad biological properties …
Benzodiazines (diazonaphthalenes with both nitrogens in the same ring) - cinnolines (1,2-benzodiazine), quinazolines (1,3-benzodiazine), …
Antileismanial activity, mechanism of action study and molecular docking of 1,4-bis(substituted benzalhydrazino)phthalazines.
Romero AH, Rodríguez N, Oviedo H, Lopez SE. Romero AH, et al. Arch Pharm (Weinheim). 2019 Jun;352(6):e1800299. doi: 10.1002/ardp.201800299. Epub 2019 Apr 23. Arch Pharm (Weinheim). 2019. PMID: 31012160
These compounds represent a disubstituted version of the 1-chloro-4-(monoaryl/heteroarylhydranizyl)phthalazine that exhibited a significant response against L. braziliensis according to our previous findings. ...A comparison of biological response was established between t …
These compounds represent a disubstituted version of the 1-chloro-4-(monoaryl/heteroarylhydranizyl)phthalazine that exhibited a signi …
Discovery of Potent and Novel Dual PARP/BRD4 Inhibitors for Efficient Treatment of Pancreatic Cancer.
Wang SP, Li Y, Huang SH, Wu SQ, Gao LL, Sun Q, Lin QW, Huang L, Meng LQ, Zou Y, Zhu QH, Xu YG. Wang SP, et al. J Med Chem. 2021 Dec 9;64(23):17413-17435. doi: 10.1021/acs.jmedchem.1c01535. Epub 2021 Nov 23. J Med Chem. 2021. PMID: 34813314
Bromodomain-containing protein 4 (BRD4) repression has been reported to elevate HR deficiency. Therefore, we designed, synthetized, and optimized a dual PARP/BRD4 inhibitor III-16, with a completely new structure and high selectivity against PARP1/2 and BRD4. ...
Bromodomain-containing protein 4 (BRD4) repression has been reported to elevate HR deficiency. Therefore, we designed, synthetized, a …
Rational design, synthesis and biological evaluation of dual PARP-1/2 and TNKS1/2 inhibitors for cancer therapy.
Xu Y, Wu H, Huang L, Zhai B, Li X, Xu S, Wu X, Zhu Q, Xu Q. Xu Y, et al. Eur J Med Chem. 2022 Jul 5;237:114417. doi: 10.1016/j.ejmech.2022.114417. Epub 2022 Apr 27. Eur J Med Chem. 2022. PMID: 35504210
Poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors are the first and most successful drugs designed to exploit the concept of synthetic lethality (SL) between PARP-1 and BRCA1/2, which provides a novel strategy for tumor treatment. ...
Poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors are the first and most successful drugs designed to exploit the concept of synthetic
Rational Design and Synthesis of Novel Dual PROTACs for Simultaneous Degradation of EGFR and PARP.
Zheng M, Huo J, Gu X, Wang Y, Wu C, Zhang Q, Wang W, Liu Y, Liu Y, Zhou X, Chen L, Zhou Y, Li H. Zheng M, et al. J Med Chem. 2021 Jun 10;64(11):7839-7852. doi: 10.1021/acs.jmedchem.1c00649. Epub 2021 May 26. J Med Chem. 2021. PMID: 34038131
A library of novel dual-targeting PROTAC molecules has been rationally designed and prepared. A convergent synthetic strategy has been utilized to achieve high synthetic efficiency. These dual PROTAC structures are characterized using trifunctional natural amino aci …
A library of novel dual-targeting PROTAC molecules has been rationally designed and prepared. A convergent synthetic strategy has bee …
Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer.
Huang SH, Cao R, Lin QW, Wu SQ, Gao LL, Sun Q, Zhu QH, Zou Y, Xu YG, Wang SP. Huang SH, et al. Eur J Med Chem. 2022 Feb 15;230:114116. doi: 10.1016/j.ejmech.2022.114116. Epub 2022 Jan 15. Eur J Med Chem. 2022. PMID: 35091172
Repression of BRD4 has been reported to significantly elevate HR deficiency and sensitize cancer cells to PARP1/2 inhibitors. Inspired by the concept of synthetic lethality, we designed, synthetized and optimized a dual PARP1/BRD4 inhibitor III-7, with a completely …
Repression of BRD4 has been reported to significantly elevate HR deficiency and sensitize cancer cells to PARP1/2 inhibitors. Inspired by th …
32 results