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On the basis of our consideration to design and to develop antitumor activities of heterocyclic compound derivatives, especially in fused ring system, we refer to the possibility of the heterocyclic extension of one of the most important steroid compounds used as a medicinal drug. The reaction of dydrogesterone with each of the malononitrile or ethylcyanoacetate containing elemental sulfur afforded thiophene derivatives  1a , b . Also, dydrogesterone was reacted with a mixture of ethylcyanoacetate–hydrazine, ethylcyanoacetae–urea, or ethylcyanoacetate–thiourea to produce pyrazole derivative  4  and pyrimidine derivatives  5a , b . Thienopyrimidine derivatives  2a – d  were introduced from the reaction of thiophene derivatives  1a , b  with either phenylisothiocyanate or benzoylisothioyanate. Furthermore, compounds  1a , b  were directed toward the reaction with ethylcyanoacetate to produce compounds  6a , b , and the last compounds  6a , b  were directed toward cyclization to obtain thienopyridine derivatives  7a , b . In addition, compounds  6a , b  were subjected to react with different carbonyl compounds, such as salicylaldehyde, cyclopentanone-elemental sulfur, malonaldehyde, and acetylacetone to produce coumarin derivatives  8a , b , fused thiophene derivatives  9a , b , and pyridine derivatives  10a – d . Isooxazole derivatives  12a , b  were afforded through the reaction of compounds  6a , b  with hydroxylamine hydrochloride. Finally, 2-pyridone derivatives  14a , b  were obtained through the reaction of compounds  6a , b  with benzoylacetonitrile. Conformation structure of the synthesized compounds was established by applying IR,  1 H NMR,  13 C NMR, and mass spectrometry, and their antitumor activity was examined. Some compounds showed promising growth inhibitory effects on the three different cell lines.

open chemistry

Design, synthesis, and biological activities of novel thiophene, pyrimidine, pyrazole, pyridine, coumarin and isoxazole: Dydrogesterone derivatives as antitumor agents