Abstract
A novel series of 4-(4-formamidophenylamino)-N-methylpicolinamide derivatives were synthesized and evaluated against different tumor cell lines. Experiments in vitro showed that these derivatives could inhibit the proliferation of two kinds of human cancer cell lines (HepG2, HCT116) at low micromolar concentrations and the most potent analog 5q possessed broad-spectrum antiproliferative activity. Experiments in vivo demonstrated that 5q could effectively prolong the longevity of colon carcinoma-burdened mice and slow down the progression of cancer cells by suppression of angiogenesis and the induction of apoptosis and necrosis.
Highlights
In a previous cell-based screening anticancer drugs, we found an active structure: 4-(4-formamidophenylamino)-N-methyl picolinamide [23,24]
Thesestructure: derivates4-(4-formamidophenylamino)-N-methyl were evaluated against different tumor anticancer we found an active cell lines by Experiments in vitro showed that mostand of synthesized the derivatives could picolinamide [23,24]
4-(4-formamidophenylamino)-N-methylpicolinamide were prepared to the general synthetic strategy illustrated derivatives in Scheme 1(5a–v) were prepared according to the general synthetic strategy illustrated in
Summary
Cancer is one of the most common causes of death and its incidence is increasing worldwide [1]. Deregulated proliferation and inhibition of apoptosis lie at the heart of all tumor development, so they present two obvious targets for therapeutic intervention in all cancers [2,3]. According to the opinion of Folkman, the growth and metastasis of neoplasms depend on new blood vessels. The diameter of neoplasms cannot exceed 2 mm without the support of new blood vessels. The targeting of cancerous blood vessels is becoming a hot topic in the development of new drugs [7,8,9,10,11,12,13]
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