Synthesis of 4-mono and 2,4-disubstituted pyrido ..

Synthesis of Novel Pyrido[3′,2′:4,5]furo[3,2-d]pyrimidine Derivatives and Their Cytotoxic Activity
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Synthesis of pyrido[2,3-d][1,2,4]triazolo ..

In summary, we have designed and synthesized a new series of 4-substituted-2-amino-pyrido[3,4-d]pyrimidine analogs as potential anticancer agents. A convenient and efficient synthetic strategy has been developed which can rapidly generate analogs with diverse substituents at the C-4 position of the core scaffold. Screening of the representative analogs using the NCI 60 cancer cell line panel has shown highly selective inhibitory effects against the growth of the UO-31 renal cancer cell line, MDA-MB-468 and MCF-7 breast cancer cell lines. Compounds 13 and 21 represent promising starting points for the development of this new compound class as molecularly targeted chemotherapeutic agents. The mechanism of action (MOA) studies to determine their cellular targets are underway. The results of our study suggest that this compound class (in particular compounds 13 and 21) has merits for further development towards potential candidates for clinical trials in the treatment of cancers.

Synthesis of Novel Pyrido[1,2-a]pyrimidine-3-carboxamide Derivatives and Their Anticancer Activity
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Eco-friendly Synthesis of Pyrido[2,3-d]pyrimidine …

T1 - Synthesis and Biological Evaluation of 2,4-Diamino-6-(arylaminomethyl)pyrido[2,3-d]pyrimidines as Inhibitors of Pneumocystis carinii and Toxoplasma gondii Dihydrofolate Reductase and as Antiopportunistic Infection and Antitumor Agents

The first major synthesis of pyridine derivatives was described in 1881 by Arthur Rudolf Hantzsch.
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A series of novel pyrido[1,2-]pyrimidine-3-carboxamide derivatives 6an were prepared starting from 2(1) pyridone 1 hydrolysis, de-carboxylation, selective -alkylation followed by rearrangement to give pyridine-2-amine 3. Compound 3 on reaction with ethoxy methylene malonic diethyl ester (EMME) under a conventional method followed by cyclization under micro wave irradiation (MWI) conditions resulted in product 5. Compound 5 on coupling with diverse substituted aliphatic amines formed title compounds 6an. All the products 6an were screened against four human cancer cell lines and compounds 6hk and n which showed promising anticancer activity have been identified.

Synthesis of Novel Pyrido[3,2- e ][1,2,4]triazolo[1,5- c ]pyrimidine Derivatives: Potent and Selective Adenosine A 3 Receptor Antagonists
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PDF Downloads : Oriental Journal of Chemistry

The crucial chlorinated intermediate, 4-chloro-8-methoxy pyrido [3,4-d]pyrimidin-2-amine, was prepared by the route depicted in . The nitration of 2-amino-4-picoline with nitric acid in concentrated sulfuric acid gave a mixture of 4-methyl-3-nitropyridin-2-amine (2) and 4-methyl-5-nitropyridin-2-amine (3) and the 3-nitro isomer was obtained by silica gel column chromatography. Then the 2-amino group was converted to a hydroxyl group with sodium nitrite (Sandmeyer condition), and compound 4 was obtained in 96% yield. Following that, chlorination (compound 5 in 78% yield), carboxylation (compound 6 in 81% yield and 7 in 96% yield) and reduction with iron (in 89% yield) were conducted in sequence to provide compound 8, which was condensed with freshly made chloroformamidine hydrochloride to elaborate compound 9 in 93% yield. After replacing the chloro with a methoxy group at the C-8 position and treating with phosphorous oxychloride, the key common intermediate, 4-chloro-8-methoxypyrido[3,4-d]pyrimidin-2-amine (11) was prepared with a satisfactory overall yield.,

ThalesNano Nanotechology Inc - Publications

A variety of synthetic strategies are known for the synthesis of fused pyrimidine systems., In the present study, the synthesis of the pyrido[4,3-d]pyrimidine heterocyclic system has been accomplished by a thermal cyclocondensation of ethyl 3-amino-2-chloroisonicotinate with chloroformamidine hydrochloride., Details are described in the following section. Also, the cytotoxicities of products were evaluated using the US National Cancer Institute’s 60 human cancer cell line (NCI 60) screen panel. Herein, we report the synthesis, cytotoxicity profile, and preliminary structure–activity relationship (SAR) of these novel compounds.