The present invention relates to 4-amino, 4-oxy, 4-thio or 4-alkyl substituted pyrrolo[3,2d]pyrimidines, furo[3,2d]pyrimidines, cyclopenta[d]pyridines, pyrrolo[2,3d]pyrimidines and furo[2,3d]pyrimidines, pharmaceutically acceptable salts, solvates and hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, such as for example P-glycoprotein inhibition and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also disclosed are these compounds for use in a method of treating tumor cells and inhibiting mitosis of cancerous cells.
本发明涉及 4-
氨基、4-氧基、4-
硫代或 4-烷基取代的
吡咯并[3,2d]
嘧啶、
呋喃并[3,2d]
嘧啶、环戊并[d]
吡啶、
吡咯并[2,3d]
嘧啶和
呋喃并[2,3d]
嘧啶、其药学上可接受的盐类、溶液和
水合物、这些化合物具有抗有丝分裂活性、抗多药耐药性活性(例如 P 糖蛋白抑制作用)和抗肿瘤活性,可抑制对
紫杉醇敏感和耐药的肿瘤细胞。还公开了这些化合物用于治疗肿瘤细胞和抑制癌细胞有丝分裂的方法。