Phytochemical investigation of the chloroform extract of Tinospora cordifolia yielded a new clerodane diterpenoid tincordin (1) along with tinosporide (2), 8-hydroxytinosporide (3), columbin (4), 8-hydroxycolumbin (5) and 10-hydroxycolumbin (6). The structure of the new compound was elucidated comprehensively using 1D and 2D NMR methods. All major clerodane diterpenoids isolated were tested for their efficacy a...
Accepted author version posted online: 05 Jun 2012 ; The synthesis of a series of novel 1,4-disubstituted 1,2,3-triazole compounds bearing a D-glucose derivative and an heteroaromatic system is described. Alkylation of isatin, 3-methyl-carbazole and one tetrahydro-gamma-carboline with propargyl bromide gave their N-propargyl derivatives in good yields. These compounds further reacted with acetylated D-glucose ...
The preparation of several alkynyl esters, derived from amino acids, coumarins and an alkynyl derivative of acetylated D-glucose is described. Eight new glycoconjugates containing the 1,2,3-triazole unit were obtained, by a click approach from the above referred alkynyl derivatives with tetracetyl-beta-D-glucosylazide, prepared in situ from alpha-acetobromoglucose.
New tetracyclic benzofurocoumarin (benzopsoralen) analogues were synthesized and their inhibitory effect on the growth of tumor cell lines was evaluated. The human tumor cell lines used were MDA MB231 (breast adenocarcinoma), HeLa (cervix adenocarcinoma) and TCC-SUP (bladder transitional cell carcinoma). The in vitro antitumor activity of the new benzopsoralens was discussed in terms of structure–activity relat...
Reaction of (dicyanomethylidene-hydrazino)benzoic acids with chloroacetonitrile, under basic conditions, gave cyanomethyl-3-(7-amino-3,5-dicyano-1H-pyrazolo[4,3-d]pyrimidin-1-yl-benzoates and para substituted cyanomethyl benzoates, in addition to the expected cyanomethyl 3-(4-amino-3,5-dicyano-1H-pyrazol-1-yl)-benzoates.
The synthesis of five new tetracyclic benzofurocoumarin (benzopsoralen) analogues is described. Their inhibitory effects on the growth of three human tumour cell lines (MDA MB 231 (breast adenocarcinoma), HeLa (cervix adenocarcinoma) and TCC-SUP (bladder transitional cell carcinoma)) were evaluated, and discussed in terms of structure–activity relationship.
Psoralens are natural products present in several plant families that are extremely toxic to a wide variety of prokaryotic and eukaryotic organisms. They are potentially active in diseases such as vitiligo, psoriasis, and several types of cancer. Following our interest on this type of compounds 1 four new psoralen analogues were prepared, 1a-1c and 1e. To synthesize 1a (R = H) the method of Harayama and Ishii w...
The preparation of b-carbolines and of three alkynyl esters, two of them derived from carbolines, is described. Two new glycoconjugates were obtained, one by a click approach from an alkynyl derivative with tetracetyl-b-D-glucosylazide and the other one by linking a carboline carboxylic acid with tetracetyl-b-D-glucosylamine.
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