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A series of novel alkylthio/sulfinyl-8 H -thieno[2,3-b]pyrrolizin-8-oximino derivatives V 1 –VIII 15 were designed and synthesized as antitumor agents. Their structures were confirmed using IR, 1 H NMR, elemental analysis, and MS. The antitumor activities of all the target compounds were tested by the MTT method in vitro against Bel-7402, HT-1080, SGC-7901, and A549 Cell Lines. Among them, compound VI 9 displayed a promising antitumor activity superior to that of Cisplatin.

A series of novel pyrazolo [4, 3-d] pyrimidin-7-ones was designed and synthesized in order to find new potent phosphodiesterase 5 inhibitors (PDE5). The structures of all the compounds were confirmed by IR, 1 H NMR and MS; their in vitro vasodilatory activities were tested on isolated rabbit aortic spiral strips. Among them, compound X3 displays a significant vasodilatory activity, which is more potent than verapamil.

A series of novel methylthio-, sulfinyl-, and sulfonyl-8H-thieno[2,3-b]pyrrolizin-8-oximino derivatives 7A-12P was designed and synthesized as anti-tumor agents. Their structures were confirmed by IR, (1)H-NMR, MS, and elemental analysis. The anti-tumor activities of all the target compounds were tested by the MTT method in vitro against Bel-7402 (human liver cancer) and HT-1080 (human fibro sarcoma) cell lines. Among them, compound 11N (IC(50) = 18.2 microM, 8.2 microM), was the most promising compound of all synthesized molecules, it was 2.5- and 3.3-times more active than cisplatin (IC(50) = 45.2 microM, 26.7 microM), respectively.

A series of novel [1,2,4]triazolo[1,5-a]pyrimidine derivatives has been designed and synthesized in order to find novel anti-tumor compounds. The structures of all the compounds were confirmed by IR, 1H-NMR, MS and elemental analysis. Their anti-tumor activities against cancer cell lines (HT-1080 and Bel-7402) were tested by the MTT method in vitro. Among them, compound 19 displayed the best anti-tumor activity with IC50 values of 12.3 microM and 6.1 microM against Bel-7402 and HT-1080 cell lines respectively.