Src is a non-receptor tyrosine kinase (TK) whose involvement in cancer, including glioblastoma (GBM), has been extensively demonstrated. In this context, we started from our in-house library of pyrazolo[3,4-d]pyrimidines that are active as and/or Bcr-Abl TK inhibitors and performed lead optimization study to discover new generation derivative suitable for targeting. We synthesized 19 compounds,...

There has been special interest in the chemistry of quinolone and pyrimidine derivatives due to their diverse biological activities such as anticonvulsant, anti-malarial agents, antibacterial, antiviral, cytostatic, antithelemintic, antigenotoxic, anti-cancer agents. These compounds are also used as targeting delayed-type hypersensivity and anti-convulsant agents. As a part of our research work...

BACKGROUND African trypanosomes are capable of both pyrimidine biosynthesis and salvage of preformed pyrimidines from the host, but it is unknown whether either process is essential to the parasite. METHODOLOGY/PRINCIPAL FINDINGS Pyrimidine requirements for growth were investigated using strictly pyrimidine-free media, with or without single added pyrimidine sources. Growth rates of wild-type...

The new histidine derivative 3-[1-[3-(9H-fluoren-9-ylmethoxycarbonylamino)-propyl]-1H-imidazol-4-yl]-2-(3-trimethylsilanyl-ethylcarboxyamino)-propionic acid methyl ester (7) has been prepared via alkylation of the histidine urea derivative (7S)-5,6,7,8-tetrahydro-7-(methoxycarbonyl)-5-oxoimidazo-[1,5-c]-pyrimidine (2) with Fmoc-protected 3-iodopropyl-amine, followed by ring opening with 2-trime...

Target molecules based on Adamantane-pyrido[2,3-d]pyrimidine derivatives were prepared. series using N-(hydroxyadamantan-1-yl)-5-(2,4-substitutedphenyl)-2-Methyl-4-Oxo-7-(2-oxo-2H-Chromen-3-yl)pyrido[2,3-d]Pyrimidine-3(4H)carboxamide (6a-j) was synthesized by reaction between 3-(2-chloroacetyl)-5-(2,4-substitutedphenyl)-2-Methyl-7-(2-Oxo-2H-Chromen-3-yl) pyrido[2,3-d]pyrimidin-4(3H)-one (5a-j) ...

this study describes the organic synthesis of 5-(2-amimo-4-styryl pyrimidine-4-yl)-4-methoxy benzofuran-6-ol (spbf) as an example of a benzofuran derivative used as a new series of amyloid imaging agents. these benzofuran derivatives may be useful amyloid imaging agents for detecting b-amyloid plagues in the brain of alzheimer’s disease. the precursor is 1-[6-hydroxy-4-methoxybenzofuran-5-yl]-p...