Synthesis and antitumor activity of some new pyrazolo[3,4-d]pyrimidine and pyrazolo[3,4-b]pyridine derivatives

Figures & data

Scheme 1 Synthesis of 6-thioxo-1-tosyl-pyrazolo[3,4-d]pyrimidine-3-carbonitriles 3-6.

Scheme 2 Synthesis of 1-tosyl-pyrazolo[3,4-d]pyrimidine-3-carbonitriles 7, 8 and 10.

Scheme 3 Synthesis of 4-amino-1-tosyl-pyrazolo[3,4-b]pyridine-3-carbonitriles 12 and 13.

Table 1 Cytotoxic activity of the synthesized compounds against epidermoid carcinoma cell line (Hep2).

Compounds	In vitro cytotoxicity IC50 (µM)
	Hep2
5-FU	41.5 ± 3.1
2	196.8 ± 13.4
3	36.9 ± 2.6
4	21.3 ± 1.6
5	55.5 ± 5.2

5-FU = 5-fluorouracil. Data are reported as means ± SD.