Repository logo
  • English
  • 中文
Log In
Have you forgotten your password?
  1. Home
  2. College of Medicine / 醫學院
  3. Clinical Laboratory Sciences and Medical Biotechnology / 醫學檢驗暨生物技術學系所
  4. Antitumor agents 283. Further elaboration of Desmosdumotin C analogs as potent antitumor agents: Activation of spindle assembly checkpoint as possible mode of action
 
  • Details

Antitumor agents 283. Further elaboration of Desmosdumotin C analogs as potent antitumor agents: Activation of spindle assembly checkpoint as possible mode of action

Journal
Bioorganic and Medicinal Chemistry
Journal Volume
19
Journal Issue
5
Pages
1816-1822
Date Issued
2011
Author(s)
Nakagawa-Goto K.
Wu P.-C.
Bastow K.F.
Yang S.-C.
SUNG-LIANG YU  
Chen H.-Y.
Lin J.-C.
Goto M.
Morris-Natschke S.L.
PAN-CHYR YANG  
Lee K.-H.
DOI
10.1016/j.bmc.2011.01.001
URI
https://scholars.lib.ntu.edu.tw/handle/123456789/502898
Abstract
In our ongoing study of the desmosdumotin C (1) series, twelve new analogues, 21-32, mainly with structural modifications in ring-A, were prepared and evaluated for in vitro antiproliferative activity against several human tumor cell lines. Among them, the 4′-iodo-3,3,5-tripropyl-4-methoxy analogue (31) showed significant antiproliferative activity against multiple human tumor cell lines with ED 50 values of 1.1-2.8 μM. Elongation of the C-3 and C-5 carbon chains reduced activity relative to propyl substituted analogues; however, activity was still better than that of natural compound 1. Among analogues with various ether groups on C-4, compounds with methyl (2) and propyl (26) ethers inhibited cell growth of multiple tumor cells lines, while 28 with an isobutyl ether showed selective antiproliferative activity against lung cancer A549 cells (ED 50 1.7 μM). The gene expression profiles showed that 3 may modulate the spindle assembly checkpoint (SAC) and chromosome separation, and thus, arrest cells at the G2/M-phase. ? 2011 Elsevier Ltd. All rights reserved.
SDGs

[SDGs]SDG3

Other Subjects
3,3,5 tripropyl 5 prenyldesmosdumotin C; 4 isobutoxy 3,3,5 tripropyldesmosdumotin C; 4 propoxy 3,3,5 tripropyldesmosdumotin C; antineoplastic agent; carbon; desmosdumotin C derivative; methyl group; natural product; paclitaxel; propane; unclassified drug; vincristine; antineoplastic activity; article; cancer cell culture; cell cycle arrest; cell cycle G2 phase; cell cycle M phase; cell proliferation; chromosome; controlled study; drug mechanism; drug potency; drug screening; drug selectivity; gene expression profiling; human; human cell; in vitro study; mitosis spindle; structure activity relation; Alkenes; Antineoplastic Agents; Cell Line, Tumor; Drug Screening Assays, Antitumor; Humans; Ketones; Mitotic Spindle Apparatus; Models, Biological; Molecular Structure; Neoplasms
Type
journal article

臺大位居世界頂尖大學之列,為永久珍藏及向國際展現本校豐碩的研究成果及學術能量,圖書館整合機構典藏(NTUR)與學術庫(AH)不同功能平台,成為臺大學術典藏NTU scholars。期能整合研究能量、促進交流合作、保存學術產出、推廣研究成果。

To permanently archive and promote researcher profiles and scholarly works, Library integrates the services of “NTU Repository” with “Academic Hub” to form NTU Scholars.

總館學科館員 (Main Library)
醫學圖書館學科館員 (Medical Library)
社會科學院辜振甫紀念圖書館學科館員 (Social Sciences Library)

開放取用是從使用者角度提升資訊取用性的社會運動,應用在學術研究上是透過將研究著作公開供使用者自由取閱,以促進學術傳播及因應期刊訂購費用逐年攀升。同時可加速研究發展、提升研究影響力,NTU Scholars即為本校的開放取用典藏(OA Archive)平台。(點選深入了解OA)

  • 請確認所上傳的全文是原創的內容,若該文件包含部分內容的版權非匯入者所有,或由第三方贊助與合作完成,請確認該版權所有者及第三方同意提供此授權。
    Please represent that the submission is your original work, and that you have the right to grant the rights to upload.
  • 若欲上傳已出版的全文電子檔,可使用Open policy finder網站查詢,以確認出版單位之版權政策。
    Please use Open policy finder to find a summary of permissions that are normally given as part of each publisher's copyright transfer agreement.
  • 網站簡介 (Quickstart Guide)
  • 使用手冊 (Instruction Manual)
  • 線上預約服務 (Booking Service)
  • 方案一:臺灣大學計算機中心帳號登入
    (With C&INC Email Account)
  • 方案二:ORCID帳號登入 (With ORCID)
  • 方案一:定期更新ORCID者,以ID匯入 (Search for identifier (ORCID))
  • 方案二:自行建檔 (Default mode Submission)
  • 方案三:學科館員協助匯入 (Email worklist to subject librarians)

Built with DSpace-CRIS software - Extension maintained and optimized by 4Science