SUBSTITUTED PYRROLO[2,3-D]DIPYRIMIDINES FOR SELECTIVELY TARGETING TUMOR CELLS WITH FR-ALPHA AND FR-BETA TYPE RECEPTORS

摘要

Pyrrolo[2,3-d]pyrimidine derivatives, and pharmaceutical acceptable salts thereof, useful in therapeutically treating patients with cancer are disclosed. These compounds selectively target folate receptors (FR) of cancerous tumor cells and inhibit purine synthesis and hence, DNA synthesis.

主权项

1. A compound, or pharmaceutically acceptable salt thereof, having a general formula 1:wherein,
R1 is hydrogen; R2 is NHR wherein R is hydrogen; A is NR′, wherein R′ is hydrogen; B is CR′R″, wherein R′ and R″ are each hydrogen; the position of the side chain on the five-membered ring is selected from the group consisting of position 5 and 6; one of X, Y, Z and Q is (CR′R″)n, wherein n is 0; and Ar is monocyclic aryl or heteroaryl ring.