Diversity oriented synthesis of benzoxanthene and benzochromene libraries via one-pot, three-component reactions and their anti-proliferative activity.
Libraries of benzoxanthenes, as well as of benzochromenes, were efficiently synthesized via one-pot, three-component reactions of 2-naphthol, aldehydes, and cyclic 1,3-diketones/malononitrile/ethyl cyanoacetate in the presence of catalytic amount of ceric ammonium nitrate (CAN) under solvent free conditions. The protocol offers rapid synthesis of structurally diverse benzoxanthenes and benzochromenes for biologically screening. All the synthesized compounds were evaluated for their anti-proliferative activity, and several compounds were exhibiting promising anti-proliferative activity.
Kumar
Atul
A
Medicinal and Process Chemistry Division, Central Drug Research Institute, CSIR, Lucknow, India. dratulsax@gmail.com
Sharma
Siddharth
S
Maurya
Ram Awatar
RA
Sarkar
Jayant
J
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis*; D001554:Benzene / Q000737:chemistry*; D001578:Benzopyrans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D049109:Cell Proliferation / Q000187:drug effects; D002522:Chlorocebus aethiops; D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D006801:Humans; D020128:Inhibitory Concentration 50; D014709:Vero Cells; D014966:Xanthenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D000970:Antineoplastic Agents; D001578:Benzopyrans; D014966:Xanthenes; D001554:Benzene