Kemnitzer, William published the artcileDiscovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 2. Structure-activity relationships of the 7- and 5-, 6-, 8-positions, Recommanded Product: 3-Morpholinophenol, the publication is Bioorganic & Medicinal Chemistry Letters (2005), 15(21), 4745-4751, database is CAplus and MEDLINE.
As a continuation of our efforts to discover and develop the apoptosis inducing 4-aryl-4H-chromenes as novel anticancer agents, the authors explored the SAR of 4-aryl-4H-chromenes with modifications at the 7- and 5-, 6-, 8-positions. It was found that a small hydrophobic group, such as NMe2, NH2, NHEt, and OMe, is preferred at the 7-position. Di-substitution at either the 5,7-positions or the 6,7-positions generally led to a large decrease in potency. Di-substitution at the 7,8-positions, in general, was found to result in potent compounds 7-NMe2, 7-NHEt, 7-OMe, and 7,8-di-NH2 analogs were found to have similar SAR for the 4-aryl group, and several 7-substituted and 7,8-di-substituted analogs were found to have similar potencies as the lead compound MX58151 (I) both as caspase activators and inhibitors of cell proliferation.
Bioorganic & Medicinal Chemistry Letters published new progress about 27292-49-5. 27292-49-5 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Benzene,Phenol, name is 3-Morpholinophenol, and the molecular formula is C10H13NO2, Recommanded Product: 3-Morpholinophenol.
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