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 Chemjournal_title
European journal of medicinal chemistryauthors
Zang Y,Lai F,Fu J,Li C,Ma J,Chen C,Liu K,Zhang T,Chen X,Zhang Ddoi
10.1016/j.ejmech.2020.112079subject
Has Abstractpub_date
2020-03-15 00:00:00pages
112079eissn
0223-5234issn
1768-3254pii
S0223-5234(20)30046-5journal_volume
190pub_type
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