دورية أكاديمية
Scaffold Hopping-Driven Optimization of 4-(Quinazolin-4-yl)-3,4-dihydroquinoxalin-2(1 H )-ones as Novel Tubulin Inhibitors.
| العنوان: | Scaffold Hopping-Driven Optimization of 4-(Quinazolin-4-yl)-3,4-dihydroquinoxalin-2(1 H )-ones as Novel Tubulin Inhibitors. |
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| المؤلفون: | Jiang L; Beijing Institute of Pharmacology and Toxicology, 27 Tai-Ping Road, Beijing 100850, China., Goto M; Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, United States., Zhu DQ; Beijing Institute of Pharmacology and Toxicology, 27 Tai-Ping Road, Beijing 100850, China., Hsu PL; Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, United States., Li KP; Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, United States., Cui M; Beijing Institute of Pharmacology and Toxicology, 27 Tai-Ping Road, Beijing 100850, China., He X; Beijing Institute of Radiation Medicine, 27 Tai-Ping Road, Beijing 100850, China., Morris-Natschke SL; Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, United States., Lee KH; Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, United States.; Chinese Medicine Research and Development Center, China Medical University and Hospital, Taichung, Taiwan., Xie L; Beijing Institute of Pharmacology and Toxicology, 27 Tai-Ping Road, Beijing 100850, China.; Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, United States. |
| المصدر: | ACS medicinal chemistry letters [ACS Med Chem Lett] 2019 Dec 30; Vol. 11 (1), pp. 83-89. Date of Electronic Publication: 2019 Dec 30 (Print Publication: 2020). |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: American Chemical Society Country of Publication: United States NLM ID: 101521073 Publication Model: eCollection Cited Medium: Print ISSN: 1948-5875 (Print) Linking ISSN: 19485875 NLM ISO Abbreviation: ACS Med Chem Lett Subsets: PubMed not MEDLINE |
| أسماء مطبوعة: | Original Publication: Washington, D.C. : American Chemical Society |
| مستخلص: | Scaffold hopping-driven lead optimizations were performed based on our prior lead 7-methoxy-4-(2-methylquinazolin-4-yl)-3,4-dihydroquinoxalin-2(1 H )-one ( 2a ) by C-ring expansion and isometric replacement of the A/B-ring, successively, aimed at finding new potential alternative drug candidates with different scaffold(s), high antitumor activity, and other improved properties to replace prior, once promising drug candidates that failed in further studies. Two series of new compounds 7 ( a-d ) and 13 ( a-j ) were synthesized and evaluated for antitumor activity, leading to the discovery of three highly potent compounds 13c , 13d , and 13e with different scaffolds. They exhibited similar high antitumor activity with single digital low nanomolar GI Competing Interests: The authors declare no competing financial interest. (Copyright © 2019 American Chemical Society.) |
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| معلومات مُعتمدة: | P30 CA016086 United States CA NCI NIH HHS; R01 CA177584 United States CA NCI NIH HHS |
| تواريخ الأحداث: | Date Created: 20200116 Latest Revision: 20210310 |
| رمز التحديث: | 20240829 |
| مُعرف محوري في PubMed: | PMC6956357 |
| DOI: | 10.1021/acsmedchemlett.9b00352 |
| PMID: | 31938468 |
| قاعدة البيانات: | MEDLINE |
Find this issue from the American Chemical Society | تدمد: | 1948-5875 |
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| DOI: | 10.1021/acsmedchemlett.9b00352 |