Yadav, Mange Ram; Chauhan, Bishram Singh; Naik, Prashant; Gandhi, Hardik; Giridhar, Rajani published the artcile< 6,7-Dimethoxyquinazolines as Potential Cytotoxic Agents: Synthesis and in vitro Activity>, Electric Literature of 5004-88-6, the main research area is quinazolinone dimethoxy preparation anticancer cytotoxicity; quinazoline dimethoxy diamino preparation antitumor.
Series of substituted 6,7-dimethoxyquinazolinones I (R1 = H, n-Bu; n = 0, 1; R2 = 4-ClC6H4, 4-MeOC6H4, etc.) and diaminoquinazolines II (R3 = 2-MeC6H4, 3-HO2CC6H4, 4-H2NSO2C6H4, etc.) were synthesized. The compounds I (R1 = n-Bu) were synthesized with the aim of increasing the lipophilicity. The cytotoxicity of the selected products was evaluated against National Cancer Institute (NCI) 60 cell panel using the NCI disease oriented antitumor screen protocol. Based on the results of this screening, it was generalized that compounds having aryl groups directly attached to the quinazoline ring are less active than those which have one atom linker between the two ring systems. Substitution with a lipophilic group like n-Bu decreased cytotoxic activity among the compounds, whereas 4-aminoquinazolines showed better activity than 4-quinazolinones. Lipophilic groups in the aromatic ring increased the cytotoxicity. The selected compounds I (R1 = H; n = 1; R2 = 4-MeOC6H4) and II (R3 = 3-ClC6H4) were found to be potential lead compounds, which could be further optimized as potential anti-neoplastic agents.
Letters in Drug Design & Discovery published new progress about Antitumor agents. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Electric Literature of 5004-88-6.
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics