Two nitrogen mustard derivatives, as well as preparation method and application therefore in tumor treatment

2013 
Novel nitrogen mustard derivatives, characterized in that: one end having a nitrogen mustard alkylating group; and the other end having a 6,7-substituted quinazoline structure, the substituents R1 located on the parent quinazoline 4, is 2 or 3 - nitrogen mustards groups; 6,7 position of the quinazoline precursor as morpholino-propoxy and methoxy. The structural formula A. Experiments show that these compounds inhibit cell cycle in G2 / M phase, it is a bifunctional alkylating agent. Experimental antitumor activity in vivo show that these compounds have good activity. Moreover, these compounds also have no drugs nitrogen mustards advantage, i.e., less toxic. At the same time, such compounds are easy to synthesize, higher overall yield. Many advantages, such compounds show has become a cancer treatment drug has great potential.
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