通过一锅三组分反应实现苯并氧杂蒽和苯并色烯库的多样性导向合成及其抗增殖活性。

Diversity oriented synthesis of benzoxanthene and benzochromene libraries via one-pot, three-component reactions and their anti-proliferative activity.

作者信息

Kumar Atul, Sharma Siddharth, Maurya Ram Awatar, Sarkar Jayant

机构信息

Medicinal and Process Chemistry Division, Central Drug Research Institute, CSIR, Lucknow, India.

出版信息

J Comb Chem. 2010 Jan-Feb;12(1):20-4. doi: 10.1021/cc900143h.

DOI:10.1021/cc900143h

PMID:19954208

Abstract

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.

摘要

在无溶剂条件下，以催化量的硝酸铈铵（CAN）为催化剂，通过2-萘酚、醛与环状1,3-二酮/丙二腈/氰基乙酸乙酯的一锅三组分反应，高效合成了苯并氧杂蒽以及苯并色烯的化合物库。该方法为生物筛选提供了结构多样的苯并氧杂蒽和苯并色烯的快速合成途径。对所有合成化合物的抗增殖活性进行了评估，几种化合物表现出有前景的抗增殖活性。