A series of 2,5,7-trisubstituted pyrimido[4,5-d]pyrimidine cyclin-dependent kinase (CDK2) inhibitors is designed and synthesized. 6-Amino-2-thiouracil is reacted with an aldehyde and thiourea to prepare the pyrimido[4,5-d]-pyrimidines. Alkylation and amination of the latter ones give different amino derivatives. These compounds show potent and selective CDK inhibitory activities and inhibit in ...

Table 1. Concentration of thiouracil in the medium. In order to ascertain whether the decrease of radioactivity in the medium is accompanied by an incorporation into nucleic acids, these were separated in the following manner: the bacterial cells were washed twice and concentrated to 50 mg wet weight/ml. They were lysed by treating with sodiumdodecylsulfate (1%) and shaken with water-saturated ...

Reports: The Award of Guggenheim Fellowships for 1944 301 Special Articles: The Effect of Adrenal Cortical and Pituitary Adrenotropic Hormones on Transplanted Leukemia in Rats: DR. JAMES B. MURPHY and DR. ERNEST STURM. Adequacy of the Essential Amino Acids for Growth of the Rat: DR. V. EVERETT KINSEY and DR. W. MORTON GRANT. Metabolic Effects of Thiouracil in Graves' Disease: MARGARET H. SLOAN ...

1. The effect of drugs that cause neutropenia has been tested upon normal bone marrow colony formation in semi-solid agar. 2. Thiouracil, methimazole and phenylbutazone do not cause inhibition whereas sodium aurothiomalate, 6-mercaptopurine and chloramphenicol cause doserelated inhibition of colony formation at or below drug concentrations found in serum during therapy. Chloramphenicol also inh...

Guanidine-based peptide nucleic acid (GPNA) monomers and oligomers containing all four natural (adenine (A), cytosine (C), guanine (G), and thymine (T)) and two unnatural (2-thiouracil (sU) and 2,6-diaminopurine (D)) nucleobases have been synthesized. Thermal denaturation study showed that GPNA oligomers containing alternate D-backbone configuration bind sequence-specifically to DNA and, when i...

To elucidate the pathogenesis of thyroid gland hypervascularity in patients with Graves' disease, we studied the expression of mRNAs for vascular endothelial growth factor (VEGF) and its receptor, Flt family, using human thyroid follicles in vitro and thiouracil-fed rats in vivo. Human thyroid follicles, cultured in the absence of endothelial cells, secreted de novo-synthesized thyroid hormone ...

Peroxidase metabolism of 2-amino-4-(5-nitro-2-fiiryl)thiazole (ANFI") was evaluated in vitro and in rivo. IH vitro metabolism of ANFT was characteristic of the hydroperoxidase activity of prostaglandin H synthase. The peroxidase inhibitors, 6-n-propyl-2-thiouracil and methimazole, significantly reduced ANFT binding to trichloroacetic acid precipitable material and glutathione conjugate formatio...