Studies on Pyrimidine Derivatives. II

Receptor Tyrosine Kinase Inhibitory Activities and Molecular Docking Studies of Some Pyrrolo[2,3-d]pyrimidine Derivatives

In this study, we aimed to determine VEGFR-2, EGFR and PDGFR-β tyrosine kinase inhibitory activities of some pyrrolo[2,3-d]pyrimidine derivatives previously synthesized and showed potent cytotoxic and apoptotic effects against several cancer cell lines by our group and to evaluate the relationships between inhibitory activities and binding properties of the active compounds by molecular docking...

Molecular docking studies on mycobacterial tuberculosis-6-oxopurine phosphoribosyltransferase EMRB with pyrimidine derivatives

Pyrimidine derivatives are associated with broad spectrum of biological activities including anti-microbial, anticancer, anti-inflammatory etc. This prompted us to use compounds containing pyrimidine moiety and to evaluate for anti microbial activity. The present study is an in silico approach that aims at finding out the potency of pyrimidine derivatives against multidrug resistant protein of ...

Pyrimidine metabolism in man. II. Studies of leukemic cells.

By Lw H. SMITH, JR., FArm A. BAKER AND MARGARET SULLIVAN I HE CENTRAL ROLE of ribonucleic acids and deoxyribonucleic acids in protein synthesis and genetic function, respectively, has led to a continued interest in their metabolism in neoplasia. A number of antineoplastic agents have been developed as structural analogs of purine or pyrimidine precursors of the nucleic acids. These agents have ...

Pyrrolo[3,2-d]pyrimidine Derivatives as Type II Kinase Insert Domain Receptor (KDR) Inhibitors: CoMFA and CoMSIA Studies

Kinase insert domain receptor (KDR) inhibitors have been proved to be very effective anticancer agents. Molecular docking, 3D-QSAR methods, CoMFA and CoMSIA were performed on pyrrolo[3,2-d]pyrimidine derivatives as non-ATP competitive KDR inhibitors (type II). The bioactive conformation was explored by docking one potent compound 20 into the active site of KDR in its DFG-out inactive conformati...

Studies on nicotinamide derivatives.