Recent advances in the structural library of functionalized quinazoline and quinazolinone scaffolds: synthetic approaches and multifarious applications.

Structure-activity relationship (SAR) study and design strategies of nitrogen-containing heterocyclic moieties for their anticancer activities.

Piperazine scaffold: A remarkable tool in generation of diverse pharmacological agents.

1-Piperazinylphthalazines as potential VEGFR-2 inhibitors and anticancer agents: Synthesis and in vitro biological evaluation.

Due to the pharmacological activities of quinazoline and quinazolinone scaffolds, it has aroused great interest in medicinal chemists for the development of new drugs or drug candidates. The pharmacological activities of quinazoline and its related scaffolds include anti-cancer, anti-microbial, anti-convulsant, and antihyperlipidaemia. Recently, molecular hybridization technology is used for the development of hybrid analogues with improved potency by combining two or more pharmacophores of bioactive scaffolds. The molecular hybridization of various biologically active pharmacophores with quinazoline derivatives resulted in lead compounds with multi-faceted biological activity wherein specific as well as multiple targets were involved. The present review summarizes the advances in lead compounds of quinazoline hybrids and their related heterocycles in medicinal chemistry. Moreover, the review also helps to intensify the drug development process by providing an understanding of the potential role of these hybridized pharmacophoric features in exhibiting various pharmacological activities.

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Recent advances in the pharmacological diversification of quinazoline/quinazolinone hybrids

Synthesis and antiproliferative activity of 4-substituted-piperazine-1-carbodithioate derivatives of 2,4-diaminoquinazoline.

Synthesis and biological evaluation of quinazolin-4(3H)-one derivatives bearing dithiocarbamate side chain at C2-position as potential antitumor agents

Synthesis and Antiproliferative Evaluation of Hybrids of Indolin-2-one and Quinazoline-4(3H)-one Linked via Imine Bond

The invention discloses a C2-bit derivative of 4(3H)-quinazolinone as shown in a general formula (I), wherein detailed definitions of R to R are shown in the specifications. Moreover, the invention further discloses a preparation method and a medicinal composition of the compound. The compound shown in the general formula (I) has the effect of inhibiting the proliferation of human lung cancer (A-549), human breast cancer (MFC-7), human colon cancer (HT29 and HCT-116) and human cervical cancer (HeLa) cells, and can be taken as an anti-tumor medicament.

C2-bit derivative of 4(3H)-quinazolinone and preparation method and application thereof

The invention discloses a 2, 4-diamino-thieno [2, 3-d] pyrimidine derivative represented as a general formula (I), wherein definitions of R and X are specified in the instruction Besides, the invention further discloses a preparation method and medical composition of the compound The compound represented as the general formula (I) has an inhibiting effect on human lung cancer (A549), human cervical carcinoma (HeLa) and human colorectal cancer (HCT-116) cell proliferation, and can be used as an antitumor medicine

Bei-Bei Mao

Papers

Synthesis and antiproliferative activity of 4-substituted-piperazine-1-carbodithioate derivatives of 2,4-diaminoquinazoline.

Synthesis and biological evaluation of quinazolin-4(3H)-one derivatives bearing dithiocarbamate side chain at C2-position as potential antitumor agents

Synthesis and Antiproliferative Evaluation of Hybrids of Indolin-2-one and Quinazoline-4(3H)-one Linked via Imine Bond

C2-bit derivative of 4(3H)-quinazolinone and preparation method and application thereof

2, 4-diamino-thieno [2, 3-d] pyrimidine derivative as well as preparation method and application thereof