Design, semisynthesis and cytotoxic activity of novel ester derivatives of betulinic acid-1,2,4 oxadiazoles.
Taking into consideration of the biological activity of betulinic acid derivatives containing a oxadiazole ring, the semisynthetic betulinic acid-1,2,4-oxadiazole esters (14-25) were synthesized starting from betulinic acid (1) and 5-(bromomethyl)-3-aryl-1,2,4-oxadiazoles (2-13) and final compounds were tested for cytotoxic activity on three human cancer cell lines in vitro. All tested compounds showed good cytotoxic activity. The structures of synthesized compounds are established based on infrared (IR), nuclear magnetic resonance (NMR), and mass spectrometry.
a Department of Chemistry , Osmania University , Hyderabad 500068 , India.
Krishna
K
Challa
b Faculty of Technology, Department of Pharmacy , Osmania University , Hyderabad 500068 , India.
M Vijaya
MV
Bhargavi
a Department of Chemistry , Osmania University , Hyderabad 500068 , India.
G L David
GL
Krupadanam
D000970:Antineoplastic Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D015394:Molecular Structure; D019906:Nuclear Magnetic Resonance, Biomolecular; D010069:Oxadiazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D053978:Pentacyclic Triterpenes; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000737:chemistry*; D000094062:Betulinic Acid
D000970:Antineoplastic Agents; D010069:Oxadiazoles; D053978:Pentacyclic Triterpenes; D014315:Triterpenes; D000094062:Betulinic Acid
1,2,4-oxadiazole; Betulinic acid; coupling; cytotoxic activity; ester; pro drug