Kumar, Rohitesh published the artcileDesign and Synthesis of a Screening Library Using the Natural Product Scaffold 3-Chloro-4-hydroxyphenylacetic Acid, Recommanded Product: 3-Chloro-4-hydroxyphenylacetic acid, the publication is Journal of Natural Products (2015), 78(4), 914-918, database is CAplus and MEDLINE.
The fungal metabolite 3-chloro-4-hydroxyphenylacetic acid (I) was utilized in the generation of a unique drug-like screening library using parallel solution-phase synthesis. A 20-membered amide library, II (R = CH2CH2CHMe2, morpholinoethyl, CH2CH2NMe2, etc.), III (R1, R2 = H, F, R3 = H, Br, Cl, F), and IV, was generated by first converting I to Me (3-chloro-4-hydroxyphenyl)acetate, then reacting this scaffold with a diverse series of primary amines via a solvent-free aminolysis procedure. The structures of the synthetic analogs II, III, and IV were elucidated by spectroscopic data anal. The structures of compounds III (R1 = F, R2 = R3 = H), IV (R1 = R2 = H, R3 = F), and the hydrate of II (R = CH2CH2NMe2) were confirmed by single X-ray crystallog. anal. All compounds were evaluated for cytotoxicity against a human prostate cancer cell line (LNCaP) and for antiparasitic activity toward Trypanosoma brucei brucei and Plasmodium falciparum and showed no significant activity at 10 μM. The library was also tested for effects on the lipid content of LNCaP and PC-3 prostate cancer cells, and it was demonstrated that the fluorobenzyl analogs IV (R1 = R2 = H, R3 = F; R1 = R3 = H, R2 = F; R1 = F, R2 = R3 = H) significantly reduced cellular phospholipid and neutral lipid levels.
Journal of Natural Products published new progress about 33697-81-3. 33697-81-3 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene,Phenol, name is 3-Chloro-4-hydroxyphenylacetic acid, and the molecular formula is C8H7ClO3, Recommanded Product: 3-Chloro-4-hydroxyphenylacetic acid.
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