Current Issue : April - June Volume : 2017 Issue Number : 2 Articles : 5 Articles
A variety of different compounds of fused uracils were prepared simply by the heating of\n6-hydrazinyl-1-methyl-, 6-hydrazinyl-1-propyl-, or 6-hydrazinyl-1,3-dipropyluracil under reflux with\nninhydrin, isatin, benzylidene malononitrile, benzylylidene ethyl cyanoacetate, benzil, and phenacyl\nbromide derivatives. The newly synthesized compounds were completely screened for antimicrobial\nand antitumor activity....
Synthesized molecules (FP1-FP12) were evaluated against five fungal species as Candida albicans, Candida glabrata,\nCandida paropsialis, Candida tropicalis SSKM, Aspergillus niger using fluconazole as standard. Synthesized molecules (FP1-FP12)\nwere evaluated against five Gram +ve and five Gram -ve bacetria such as Bacillus cereus (+ve), Staphaylococcus saprophyticus\n(+ve), Streptococcus gordoni (+ve), Bacillus subtilis (+ve), Staphylococcus aureus (+ve) and Escherichia coli (-ve), Salmonella\ntyphimurium (-ve), Salmonella enterica (-ve), Proteus mirabilis (-ve), Pseudomonas aeruginosa (-ve) using tetracycline as standard.\nFP4 and FP10 were susceptible towards Candida albicans and Candida glabrata respectively. Except FP4 and FP10, all the\nmolecules showed dose dependent susceptible criteria against fungi. Among the synthesized molecules, FP6 was the best\nmolecule against gram +ve bacteria Bacillus subtilis, Staphylococcus aureus. FP10 was the best molecule against gram -ve\nbacteria Escherichia coli, Salmonella enterica....
The class of tubuline inhibitors is still not very well understood. This category shows potential in several classes of\ndrugs. We have exploited the nucleus for potential tubuline inhibitors. Chemical compounds that target microtubules and inhibit\nthe normal function of the mitotic spindle, have proven to be one of the best classes of cancer chemotherapeutic drugs available\nto date. Recently, combretastatin derivatives have therefore gained intense interest as potential antiproliferative agents. We\nhave used the scaffold of azetidinones to prepare structural analogues of combretastatin. A series of 1, 4 disubstituted 3 chloro 2\nazetidinones was designed using Surflex Dock (Tripos Inc.) software on the crystal structure of Tubuline (PDB entry-1SA0).\nGreen chemical synthesis of the designed series of 2-azetidinone analogues of combretastatin was undertaken using different\nsubstituted aromatic anilines and aldehydes as starting materials. The finished products have been characterized by melting\npoint, solubility and TLC and spectral analysis. The compounds have been tested for preliminary antiproliferative activity by a\nrapid, easy to perform assay method on Vigna radiata beans. The compounds have exhibited potential as anticancer activity....
Synthesis of 1, 3, 4-oxadiazole derivatives have attracted considerable attention in view of therapeutic applications. In the present research work, a series of 6-(5-methyl-1-phenyl-1H-1,2,3-triazol-4-yl)-3aryl/heteryl[1,2,4]triazolo[3,4-\nb][1,3,4]oxadiazole compounds was synthesized by treating 1-[5-(5-methyl-1-phenyl-1H-1,2,3-triazol-4-yl)-1,3,4-oxadiazol-2-\nyl] hydrazine with the corresponding acid chlorides. All the synthesized compounds have been characterized by using elemental\nanalysis, FT-IR, 1H NMR, 13C NMR spectroscopy and further supported by mass spectroscopy. Purity of all the compounds has\nbeen checked on thin layer chromatographic plate and HPLC technique. All the synthesized compounds were screened for their\nin-vitro anthelmintic and anti-microbial activity by standard methods. The compounds exhibited significant antimicrobial and\nanthelmintic activities. These compounds can be further exploited to get the potent lead compounds. The detailed synthesis and\nthe antimicrobial and anthelmintic screening of the new compounds were reported....
We report herein the design and synthesis of a series of novel 5-bromo-7-azaindolin-2-one\nderivatives containing a 2,4-dimethyl-1H-pyrrole-3-carboxamide moiety. These newly synthesized\nderivatives were evaluated for in vitro activity against selected cancer cell lines by MTT assay. Results\nrevealed that some compounds exhibit broad-spectrum antitumor potency, and the most active\ncompound 23p (IC50: 2.357ââ?¬â??3.012 Ã?¼M) was found more potent than Sunitinib (IC50: 31.594ââ?¬â??49.036 Ã?¼M)\nagainst HepG2, A549 and Skov-3, respectively....
Loading....