Novel nitric oxide-releasing derivatives of triptolide as antitumor and anti-inflammatory agents: Design, synthesis, biological evaluation, and nitric oxide release studies.

Abstract:

:A series of novel triptolide/furoxans hybrids were designed and synthesized as analogues of triptolide, which is a naturally derived compound isolated from the thunder god vine (Tripterygium wilfordii Hook. F). Some of these synthesized compounds exhibited antiproliferative activities in the nanomolar range. Among them, compound 33 exhibited both good antiproliferative activity and NO-releasing ability and the acute toxicity of compound 33 decreased more than 160 times (LD50 = 160.9 mg/kg) than triptolide. Moreover, compound 33 significantly inhibited the growth of melanoma at a low dose (0.3 mg/kg) and showed strong anti-inflammatory activity in vitro and in vivo. These results indicate that compound 33 could be a promising candidate for further study.

journal_name

Eur J Med Chem

authors

Zang Y,Lai F,Fu J,Li C,Ma J,Chen C,Liu K,Zhang T,Chen X,Zhang D

doi

10.1016/j.ejmech.2020.112079

subject

Has Abstract

pub_date

2020-03-15 00:00:00

pages

112079

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(20)30046-5

journal_volume

190

pub_type

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