Synthesis and anti-HIV activities of phorbol derivatives

	Synthesis and anti-HIV activities of phorbol derivatives
	Huang, XL; Tang, CR; Huang, XS; Yang, Y; Li, QR; Ma, MD; Zhao, L; Yang, LM; Cui, YD; Zhang, ZQ; Zheng, YT; Zhang, J
	2024
发表期刊	CHINESE JOURNAL OF NATURAL MEDICINES
ISSN	2095-6975
卷号	22 期号:2 页码:146-160
摘要	In this study, 37 derivatives of phorbol esters were synthesized and their anti -HIV -1 activities evaluated, building upon our previous synthesis of 51 phorbol derivatives. 12-Para-electron-acceptor-trans-cinnamoyl-13-decanoyl phorbol derivatives stood out, demonstrating remarkable anti -HIV -1 activities and inhibitory effects on syncytia formation. These derivatives exhibited a higher safety index compared with the positive control drug. Among them, 12-(trans-4-fluorocinnamoyl)-13-decanoyl phorbol, designated as compound 3c, exhibited the most potent anti -HIV -1 activity (EC50 2.9 nmol center dot L-1, CC50/EC50 11 117.24) and significantly inhibited the formation of syncytium (EC50 7.0 nmol center dot L-1, CC50/EC50 4891.43). Moreover, compound 3c is hypothesized to act both as an HIV -1 entry inhibitor and as an HIV -1 reverse transcriptase inhibitor. Isothermal titration calorimetry and molecular docking studies indicated that compound 3c may also function as a natural activator of protein kinase C (PKC). Therefore, compound 3c emerges as a potential candidate for developing new anti -HIV drugs.
收录类别	sci
语种	英语
文献类型	期刊论文
条目标识符	http://ir.kiz.ac.cn/handle/152453/14201
专题	科研部门_分子免疫药理学（郑永唐）
推荐引用方式 GB/T 7714	Huang, XL,Tang, CR,Huang, XS,et al. Synthesis and anti-HIV activities of phorbol derivatives[J]. CHINESE JOURNAL OF NATURAL MEDICINES,2024,22(2):146-160.
APA	Huang, XL.,Tang, CR.,Huang, XS.,Yang, Y.,Li, QR.,...&Zhang, J.(2024).Synthesis and anti-HIV activities of phorbol derivatives.CHINESE JOURNAL OF NATURAL MEDICINES,22(2),146-160.
MLA	Huang, XL,et al."Synthesis and anti-HIV activities of phorbol derivatives".CHINESE JOURNAL OF NATURAL MEDICINES 22.2(2024):146-160.

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