75 documents found, page 1 of 8

Novel benzopsoralen analogues : synthesis, biological activity and molecular do...

New benzopsoralen analogues were synthesized and their inhibitory effect on the growth of tumourtumour cell lines (MDA MB231 and TCC-SUP) was evaluated. The in vitro antitumour activity of the new benzopsoralen analogues was discussed in terms of structure–activity relationship. Molecular docking studies with human-CYP2A6 enzymes were also carried out with the synthesized compounds to evaluate the potential of ...

Synthesis of novel psoralen analogues and their in vitro antitumor activity

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...

A new anti-feedant clerodane diterpenoid from tinospora cordifolia

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...

Synthesis of novel Glycoconjugates derived from Alkynyl heterocycles through a ...

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 with the azide group in position 1, to give three fina...

Synthesis of glycoconjugates containing a 1,2,3-triazole unit

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.

Toxicological evaluation of new tacrine analogues from 4-amino-1H-pyrrole-3-car...

Synthesis of 4-amino-3,5-dicyano-arylpyrazoles : part 2 : isolation and charact...

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.

Studies on the reaction of morita-baylis-hillman with indole and carbazole deri...

Tacrine and its analogues impair mitochondrial function and bioenergetics : a l...

Tacrine is an acetylcholinesterase inhibitor used as cognitive enhancer in Alzheimer's disease treatment. However, the low therapeutic efficiency and the high incidence of side effects have limited its clinical use. In the present study, the molecular mechanisms underlying the brain activity of tacrine and two novel tacrine analogues (T1, T2) were approached focusing on three aspects: i) effects on brain cholin...

Synthesis of novel benzofurocoumarin analogues and their anti-proliferative eff...

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.