Evaluation of in vitro and in vivo Cytotoxic Activities and Kinase Inhibition of Newly Synthesized Cyclo (Nα-Dinicotinoyl)-Bis-[(L-Valinyl)-L-Lysine Methyl Ester]

222-225Cancer is a major risk disease affecting human survival. The pharmaceutical companies are continuing searching for new drug candidates with promising anticancer activities, and reduced side effects. The current work aimed at synthesized a new tripeptide with potential pharmacological properties. L-Valine methyl ester was used to prepare cyclo (Nα-dinicotinoyl)-bis-[(L-valinyl)-L-lysine methyl ester. The new compound revealed promising in vitro cytotoxic activities against different neuroblastoma, cervical carcinoma, fibrosarcoma as well as hepatocellular carcinomas. Furthermore, we also found that the obtained IC50 of the compound decreased by about 50% during its in vivo anti-prostate cancer evaluation. Furthermore, the mechanism of action studies proposes that the new prepared derivative affects cancer cells trough the inhibition of VEGFR-2 kinase enzyme

Antiproliferative Activities of Cyclo (Nα-pyrido)-bis-[(L-valinyl)-L-ornithine] and its in vitro anti-VEGFR-2 Inhibition

333–336Research is continuing for synthesizing new molecules with potent pharmacological effects against cancer. In the current work we prepared a new tripeptide and investigated its in vitro as well as in vivo antiproliferative effects. Firstly, cyclo (Nα-pyrido)-bis-[(L-valinyl)-L-ornithine] was prepared and then tested against 17 different cancer cell lines. Results showed that the prepared compound showed increased cytotoxic effects (in terms of decreased IC50 value), which reached about 20.3, 28.1, 18.3 and 72.3% against RKOP27, K561, GOTO, HT1080 cell lines, respectively, in comparison to standard positive controls. Furthermore, cancer cell viability was probably affected through VEGFR-2 kinase inhibition

Evaluation of in vitro and in vivo Cytotoxic Activities and Kinase Inhibition of Newly Synthesized Cyclo (Nα-Dinicotinoyl)-Bis-[(L-Valinyl)-L-Lysine Methyl Ester]

Cancer is a major risk disease affecting human survival. The pharmaceutical companies are continuing searching for new drug candidates with promising anticancer activities, and reduced side effects. The current work aimed at synthesized a new tripeptide with potential pharmacological properties. L-Valine methyl ester was used to prepare cyclo (Nα-dinicotinoyl)-bis-[(L-valinyl)-L-lysine methyl ester. The new compound revealed promising in vitro cytotoxic activities against different neuroblastoma, cervical carcinoma, fibrosarcoma as well as hepatocellular carcinomas. Furthermore, we also found that the obtained IC50 of the compound decreased by about 50% during its in vivo anti-prostate cancer evaluation. Furthermore, the mechanism of action studies proposes that the new prepared derivative affects cancer cells trough the inhibition of VEGFR-2 kinase enzyme

Antiproliferative Activities of Cyclo (Nα-pyrido)-bis-[(L-valinyl)-L-ornithine] and its in vitro anti-VEGFR-2 Inhibition

Research is continuing for synthesizing new molecules with potent pharmacological effects against cancer. In the current work we prepared a new tripeptide and investigated its in vitro as well as in vivo antiproliferative effects. Firstly, cyclo (Nα-pyrido)-bis-[(L-valinyl)-L-ornithine] was prepared and then tested against 17 different cancer cell lines. Results showed that the prepared compound showed increased cytotoxic effects (in terms of decreased IC50 value), which reached about 20.3, 28.1, 18.3 and 72.3% against RKOP27, K561, GOTO, HT1080 cell lines, respectively, in comparison to standard positive controls. Furthermore, cancer cell viability was probably affected through VEGFR-2 kinase inhibition

Synthesis and Antimicrobial Activities of Some New Synthesized Imide and Schiff's Base Derivatives

A series of 2,6-bis(substituted thiazolopyrimi-dinyl) pyridine (2a,b) and corresponding Schiff's bases (3a–j) were synthesized from 2,6-bis-(3-amino-2-methyl-4-oxo-9-substituted-3,4-dihydropyrido-[30,20 : 4,5]-thieno[3,2-d]pyrimidin-7-yl)pyridines (1a,b) as starting materials. The compounds 1a,b were reacted with 2,3,4,5-tetrachlorophthalic anhydride in glacial acetic acid to give the corresponding bis-imides (2a,b). But they are treated with aromatic aldehydes in refluxing ethanol to afford the Schiff’s base derivatives (3a–j). The antimicrobial screening showed that many of these newly synthesized compounds had good antimicrobial activities comparable to streptomycin and fusidic acid as positive controls. The detailed synthesis, spectroscopic data, and antimicrobial activities of the synthesized compounds were reported

2-Amino-4-(4-chlorophenyl)-4H-chromeno[8,7-b]pyridine-3-carbonitrile

The asymmetric unit of the title compound, C19H12ClN3O, contains two molecules with similar conformations. The 14 non-H atoms comprising the 4H-chromeno[8,7-b]pyridine residue are essentially coplanar (r.m.s. deviations = 0.037 and 0.042 Å for the two molecules) and the main difference between them is seen in the twist about the bond linking the main residue to the attached chlorobenzene rings [dihedral angles = 79.01 (12) and 76.22 (11)° for the two molecules]. Zigzag supramolecular chains along the a-axis direction mediated by amino–pyridine N—H...N hydrogen bonds feature in the crystal packing; these are connected into a three-dimensional architecture by C—H...π interactions and Cl...Cl contacts [Cl...Cl = 3.3896 (14) Å]