Synthesis and biological evaluation of novel tricyclic matrinic derivatives as potential anti-filovirus agents
Twenty-six novel tricyclic sophoridinic and matrinic derivatives containing a common chlorinated benzene fragment were designed, synthesized and evaluated for their anti-ebolavirus (EBOV) activities. Structureactivity relationship analysis indicated: (i) 12N-dichlorobenzyl motif was beneficial for...
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| Main Authors: | , , , , , , , , , |
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| Format: | Book |
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Elsevier,
2018-07-01T00:00:00Z.
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| LEADER | 00000 am a22000003u 4500 | ||
|---|---|---|---|
| 001 | doaj_af45ee4cf6b34b58a77f81d7f2b04fab | ||
| 042 | |a dc | ||
| 100 | 1 | 0 | |a Xin Zhang |e author |
| 700 | 1 | 0 | |a Qiang Liu |e author |
| 700 | 1 | 0 | |a Qianqian Li |e author |
| 700 | 1 | 0 | |a Yinghong Li |e author |
| 700 | 1 | 0 | |a Zhandong Liu |e author |
| 700 | 1 | 0 | |a Hongbin Deng |e author |
| 700 | 1 | 0 | |a Sheng Tang |e author |
| 700 | 1 | 0 | |a Yanxiang Wang |e author |
| 700 | 1 | 0 | |a Youchun Wang |e author |
| 700 | 1 | 0 | |a Danqing Song |e author |
| 245 | 0 | 0 | |a Synthesis and biological evaluation of novel tricyclic matrinic derivatives as potential anti-filovirus agents |
| 260 | |b Elsevier, |c 2018-07-01T00:00:00Z. | ||
| 500 | |a 2211-3835 | ||
| 500 | |a 10.1016/j.apsb.2018.01.006 | ||
| 520 | |a Twenty-six novel tricyclic sophoridinic and matrinic derivatives containing a common chlorinated benzene fragment were designed, synthesized and evaluated for their anti-ebolavirus (EBOV) activities. Structureactivity relationship analysis indicated: (i) 12N-dichlorobenzyl motif was beneficial for the activity; (ii) the chiral configuration at C5 atom might not affect the activity much. Among the target compounds, compound 7d exhibited the most potent potency against EBOV with an IC50 value of 5.29 μmol/L and an SI value of over 37.8. Further in vivo anti-EBOV assay of 7d identified its high effectiveness, and in vivo anti-MARV assay of 7d suggested its inspiring broad-spectrum anti-filovirus activity. The results provided powerful information on further strategic optimization and development of this kind of compounds against filoviruses. KEY WORDS: Sophoridinic, Matrinic, Structure−activity relationship, EBOV, Filovirus | ||
| 546 | |a EN | ||
| 690 | |a Therapeutics. Pharmacology | ||
| 690 | |a RM1-950 | ||
| 655 | 7 | |a article |2 local | |
| 786 | 0 | |n Acta Pharmaceutica Sinica B, Vol 8, Iss 4, Pp 629-638 (2018) | |
| 787 | 0 | |n http://www.sciencedirect.com/science/article/pii/S2211383517305130 | |
| 787 | 0 | |n https://doaj.org/toc/2211-3835 | |
| 856 | 4 | 1 | |u https://doaj.org/article/af45ee4cf6b34b58a77f81d7f2b04fab |z Connect to this object online. |