Article

Synthesis and biological evaluation of andrographolide derivatives as potent anti-HIV agents.

Center of Drug Discovery, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, P. R. China.
Archiv der Pharmazie (impact factor: 1.71). 05/2012; 345(8):647-56. DOI:10.1002/ardp.201200008
Source: PubMed

ABSTRACT In an attempt to develop potent anti-HIV drugs, 20 andrographolide derivatives were designed, synthesized, and evaluated for their in vitro anti-HIV activity. The screening results revealed that five compounds showed potent anti-HIV activities with therapeutic indices (TI) above 10. The most promising compound 6f shows a significant TI close to 34.07, with the potency to be a new lead.

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Keywords

new lead
 
potent anti-HIV activities
 
potent anti-HIV drugs
 
screening results
 
synthesized
 
therapeutic indices
 
vitro anti-HIV activity
 

Chunlei Tang