| In vitro: |
| Planta Medica, 2012, 78(11):1284-1284. | | Synthesis and determination of antimycobacterial activity of tryptanthrine, vasicine, vasicinone and derivatives thereof.[Reference: WebLink] |
METHODS AND RESULTS:
We describe the first application of the Niementowski quinazoline synthesis for the synthesis of vasicinone 3 (Fig.1), an alkaloid from Adhatoda vasica, a traditionally used plant in India for the treatment of respiratory diseases such as asthma and tuberculosis.
CONCLUSIONS:
This straightforward 2-step synthesis is an attractive basis for further medicinal chemistry work on vasicinone. Vasicine, vasicinone, deoxyvasicinone and deoxyvasicine were tested against Mycobacterium vaccae, a non-pathogenic mycobacterium closely related to Mycobacterium tuberculosis. Tryptanthrin, a related indoloquinazolinone from Strobilanthes cusia, showed antimycobacterial and antifungal activity as well as anti-proliferative activity. |
|
Cell. 2018 Jan 11;172(1-2):249-261.e12. doi: 10.1016/j.cell.2017.12.019.IF=36.216(2019)
Cell Metab. 2020 Mar 3;31(3):534-548.e5. doi: 10.1016/j.cmet.2020.01.002.IF=22.415(2019)
Mol Cell. 2017 Nov 16;68(4):673-685.e6. doi: 10.1016/j.molcel.2017.10.022.IF=14.548(2019)
ACS Nano. 2018 Apr 24;12(4): 3385-3396. doi: 10.1021/acsnano.7b08969.IF=13.903(2019)
Nature Plants. 2016 Dec 22;3: 16206. doi: 10.1038/nplants.2016.205.IF=13.297(2019)
Sci Adv. 2018 Oct 24;4(10): eaat6994. doi: 10.1126/sciadv.aat6994.IF=12.804(2019)
