2. Academic Validation
  3. Synthesis and anti-tumor activity of novel combretastatins: combretocyclopentenones and related analogues

Synthesis and anti-tumor activity of novel combretastatins: combretocyclopentenones and related analogues

  • Bioorg Med Chem Lett. 2002 Aug 5;12(15):1955-8. doi: 10.1016/s0960-894x(02)00321-9.
Nguyen-Hai Nam 1,  Yong Kim,  Young-Jae You,  Dong-Ho Hong,  Hwan-Mook Kim,  Byung-Zun Ahn
Affiliations

Affiliation

  • 1 College of Pharmacy, Chungnam National University, Taejon 305-764, Republic of Korea.
PMID: 12113817 DOI: 10.1016/s0960-894x(02)00321-9
Abstract

A series of 2-(3,4,5-trimethoxyphenyl)-3-arylcyclopent-2-ene-1-ones (8a-8e) and their related analogues, including pentenone 9a, pentenol 10a, pentene 12a, and furane 15, were synthesized and evaluated for cytotoxicity against murine and human tumor cell lines. Compounds 8a-c, 8e and 9a showed strong cytotoxicity with IC(50) values in the range of 8-34ng/mL. Compound 8e exhibited significant anti-tumor activity in BDF1 mice bearing Lewis lung carcinoma cells with an inhibition ratio of 59%.

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