Semisynthesis and cytotoxic activities of andrographolide analogues.
Andrographolide 1, a diterpenoid lactone of the plant Andrographis paniculata, known to possess antitumour activity in in vitro and in vivo breast cancer models was subjected to semisynthesis leading to the preparation of a number of novel compounds. These compounds exhibited in vitro antitumour activity with moderate to excellent growth inhibition against MCF-7 (breast) and HCT-116 (colon) cancer cells. Compounds 3,19-(2-chlorobenzylidene)andrographolide(5), 3,19-(3-chlorobenzylidene)andrographolide(6), 3,19-(3-fluorobenzylidene) andrographolide(7), 3,19-(4-fluorobenzylidene)andrographolide(8), 3,19-(2-fluorobenzylidene)andrographolide(10), 3,19-(2-chloro-5-nitrobenzylidene)andrographolide (21), 3,19-(4-chlorobenzylidene)andrographolide(30) and 3,19-(2-chloro-4-fluorobenzylidene) andrographolide(31) were also screened against 60 NCI (National Cancer Institute, USA) human tumour cell lines derived from nine cancer cell types.
Jada
Srinivasa Rao
SR
Clinical Pharmacology Laboratory, Division of Medical Sciences, National Cancer Centre, 11 Hospital Drive, 169610, Singapore.
Hamzah
Ahmad Sazali
AS
Lajis
Nordin Haji
NH
Saad
Mohammad Said
MS
Stevens
Malcolm F G
MF
Stanslas
Johnson
J
D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D045744:Cell Line, Tumor; D004224:Diterpenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D013329:Structure-Activity Relationship
D000972:Antineoplastic Agents, Phytogenic; D004224:Diterpenes; C030419:andrographolide