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Molecules 2018, 23(12), 3216; https://doi.org/10.3390/molecules23123216

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

1
Department of Chemistry, Yunnan Normal University, Kunming 650092, Yunnan, China
2
State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Kunming 650201, Yunnan, 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)
PDF [322 KB, uploaded 5 December 2018]   |   Review Reports

Abstract

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.
Keywords: ent-kaurane-type diterpenoid derivatives; antitumor; synthesis ent-kaurane-type diterpenoid derivatives; antitumor; synthesis
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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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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