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.
Highlights
Aggressive tumors are a major cause of death worldwide, accounting for 8.8 million deaths each year, and are estimated to cause 9.6 million deaths in 2018
(IsoA) [9], longikaurin [10], xerophilusins [11] (Figure 1, 1–4), which have been studied for anti-tumor activity
In the the preceding preceding letter letter we we reported reported the the synthesis synthesis and and biological biological evaluation evaluation of aa series series of of eriocalyxin eriocalyxin B
Summary
Aggressive tumors are a major cause of death worldwide, accounting for 8.8 million deaths each year, and are estimated to cause 9.6 million deaths in 2018. 70% of deaths from cancer occur in low- and middle-income countries, according to the World Health Organization (WHO) [1]. Isodon genus members have been promising leads due to their extensive pharmacological and physiological effects, such as inhibition of hepatitis viral replication [3] and bacterial infections of the lung or gut [4], as well as its antimalaria [5], antiinflammatory [6], and anti-tumor properties [7]. Over 1200 ent-Kaurane-type diterpenoids with highly compact polycyclic ring systems have been isolated from Isodon genus, notably the compounds oridonin [8]. Natural Diterpenoid Isoferritin A (IsoA) [9], longikaurin [10], xerophilusins [11] (Figure 1, 1–4), which have been studied for anti-tumor activity. The use of these natural diterpenoids for anti-tumor was hampered by its moderate potency and complex oxygenated diterpenoid scaffold
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