Chemical Biology & Drug Design

Three linear peptides were synthesised by changing the amino acid sequence of  RGD motif and radiolabeled with freshly prepared [^99mTc(CO)₃(H₂O)₃]⁺ precursor (yield ˜ 97%). Radiolabeled peptides were substantially stable up to 24 h when incubated with saline, serum and histidine solution (10^-2 M), also exhibited significant and rapid internalization in both EAC and α_vβ₃-positive B16F10 mouse melanoma cell line. Fast blood clearance, rapid urinary excretion and significantly high tumor to muscle ratios are encouraging enough to carry out further experiments for targeting tumor.

The one pot procedure for the efficient synthesis of a small library of Novel triazolo-benzoxazepine. These comp ounds were evaluated for anticancer activity against three different cancer lines(Neura 2a, Hek 293, Hep G2). The phase-contrast images, fluorescent microscope images and confocal images unambiguously confirm the cell-death.

The number of hemin conjugates with amino acids and branched peptides were synthesized. High antibacterial activity of synthesized compounds against Gram positive bacteria including methicillin - and vancomycin-resistant strains was shown. Hemolytic and cytotoxic assays indicated that majority of synthesized conjugates possess lower toxicity and hemolytic activity than hemin.

Using a strategy that combines synthetic chemistry, binding assays and a set of computational approach, we designed a series of indolebutylamine (IBA) derivatives as a new type of highly selective D3R liands. Molecular determinants critical to the binding specificity and selectivity of D3R were identified and the SAR was investigated to understand the recognition of this type of D3R ligands.