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Molecules 2018, 23(12), 3216;

Synthesis of Novel ent-Kaurane-Type Diterpenoid Derivatives Effective for Highly Aggressive Tumor Cells

Department of Chemistry, Yunnan Normal University, Kunming 650092, China
State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Kunming 650201, China
Authors to whom correspondence should be addressed.
Received: 19 November 2018 / Revised: 28 November 2018 / Accepted: 4 December 2018 / Published: 5 December 2018
(This article belongs to the Section Bioorganic Chemistry)
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We have designed and synthesized 6 ent-Kaurane-type diterpenoid derivatives containing α,β-unsaturated ketone moieties. In vitro, activity was evaluated against three human tumor cell lines and a rat myogenic cell line (HepG2, NSCLC-H292, SNU-1040, L6) by MTT assay. All the tested compounds exhibited comparable or higher activity than DDP and eriocalyxin B. Compounds 16, 17 and 18 are promising anti-tumor leads due to their cytotoxic potencies and higher selectivity, with SI values of 161.06, 47.80 and 128.20, respectively. View Full-Text
Keywords: ent-kaurane-type diterpenoid derivatives; antitumor; synthesis ent-kaurane-type diterpenoid derivatives; antitumor; synthesis

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Hu, Y.; Li, X.-N.; Ma, Z.-J.; Puno, P.-T.; Zhao, Y.; Zhao, Y.; Xiao, Y.-Z.; Zhang, W.; Liu, J.-P. Synthesis of Novel ent-Kaurane-Type Diterpenoid Derivatives Effective for Highly Aggressive Tumor Cells. Molecules 2018, 23, 3216.

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